TY - JOUR. T1 - Ethylcholine mustard aziridinium blocks the axoplasmic transport of acetylcholinesterase in cholinergic nerve fibres of the rat. AU - Kása, P.. AU - Hanin, I.. PY - 1985/7. Y1 - 1985/7. N2 - A cholinotoxin, ethylcholine mustard aziridinium ion, (AF64A) specifically and ireversibly blocks the intraaxonal transport of acetylcholinesterase in the rat. Impairment of the transport of this enzyme in the septo-hippocampal cholinergic fibres and in the sciatic nerve has been studied, using different doses of AF64A. It is demonstrated that the effect on the axonal transport is dose-dependent, but is not related to the mode of drug application. AF64A thus may exert its neurotoxic effects on cholinergic neurons at several target sites of action. In addition to the localized presynaptic mechanisms, it may also be compromising cholinergic function by inhibiting axonal transport in vivo.. AB - A cholinotoxin, ethylcholine mustard aziridinium ion, (AF64A) specifically and ireversibly blocks ...

article{1234402, author = {Dhooghe, Matthias and Kenis, Sara and Vervisch, Karel and Lategan, Carmen and Smith, Peter and Chibale, Kelly and De Kimpe, Norbert}, issn = {0223-5234}, journal = {EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY}, keyword = {Aziridinium salts,Aziridines,Ring opening,Triaminopropanes,Antimalarial agents,INTERMEDIATE AZIRIDINIUM SALTS,PLASMODIUM-FALCIPARUM,PURINE DERIVATIVES,CHIRAL AZIRIDINES,1-ALKYL-2-(BROMOMETHYL)AZIRIDINES,CHEMOTHERAPY,EPOXIDES,POTENT,ASSAY,IONS}, language = {eng}, number = {2}, pages = {579--587}, title = {Synthesis of 2-(aminomethyl)aziridines and their microwave-assisted ring opening to 1,2,3-triaminopropanes as novel antimalarial pharmacophores}, url = {http://dx.doi.org/10.1016/j.ejmech.2010.11.037}, volume = {46}, year = {2011 ...

Binary ethylenimine (BEI) is a preparation of aziridine. It can be produced by heating bromoethylamine hydrobromide or 2-aminoethyl hydrogen sulfate in the presence of sodium hydroxide (Gabriel method). It contains at least one three-membered ring which is very reactive because of the ring strain. It is used to inactivate the foot-and-mouth disease virus in vaccines for cattle, as well as other viruses and mycoplasma in blood samples. Contrary to early assumptions that ethylenimines only modified nucleic acids, it was found that trimeric ethyleimine also alters proteins in virus preparations, especially at higher pH values. The modification of the proteins affected viral particle uptake into cells. This should be taken into consideration when using BEI and other ethyleneimines as well. BEI is very hazardous since it attacks nucleic acids and proteins as described above. It can be neutralised by sodium thiosulfate; the thiosulfate is a nucleophile which opens the three-membered ring. The presence ...

S)-3-Amino-2-(1-hydroxy-2,2-dimethylprop-1-yl)-quinazolin-4(3H)-one (Q*NH2) was prepared from (L)-tert-leucine and its 3-acetoxyamino derivative (Q*NHOAc) used to aziridinate a range of alkenes. In the presence of titanium (IV) tert-butoxide, Q*NHOAc was found to convert styrene, indene, butadiene and tert-butyl acrylate with complete diastereoselectivity into the corresponding N-Q* substituted aziridines in good yield; aziridination of methyl acrylate and -methylstyrene was also highly diastereoselective. In the absence of titanium (IV) tert-butoxide, aziridination proceeded with poor diastereoselectivity in every case.;The quinazolinone (Q*) ring has proved to be invaluable in directing or assisting the course of ring-opening of the N-(Q*) aziridines produced above. Thus Q* as a substituent on nitrogen was found to be sufficiently electron-withdrawing to activate the aziridine ring towards attack by nucleophiles in the absence of acid. The C-4 carbonyl oxygen of the quinazolinone (Q*) was ...

article{1943629, abstract = {The difference in reactivity between the activated 2-bromomethyl-1-tosylaziridine and the nonactivated 1-benzyl-2-(bromomethyl)aziridine with respect to sodium methoxide was analyzed by means of DFT calculations within the supermolecule approach, taking into account explicit solvent molecules. In addition, the reactivity of epibromohydrin with regard to sodium methoxide was assessed as well. The barriers for direct displacement of bromide by methoxide in methanol are comparable for all three heterocyclic species under study. However, ring opening was found to be only feasible for the epoxide and the activated aziridine, and not for the nonactivated aziridine. According to these computational analyses, the synthesis of chiral 2-substituted 1-tosylaziridines can take place with inversion (through ring opening/ring closure) or retention (through direct bromide displacement) of configuration upon treatment of the corresponding 2-(bromomethyl)aziridines with 1 equiv of a ...

Several highly selective biochemical markers were used to assess the persistent central cholinergic dysfunction which accompanies administration of the cholinergic neurotoxin ethylcholine mustard aziridinium ion (AF64A). Rats received a single bilateral intracerebroventricular injection of AF64A (3 nmol/3 microliter/side) or vehicle and measurements were carried out in the cerebral cortices, hippocampi and corpora striata at 7 and 21 days postinjection. The drug binding sites of muscarinic cholinergic receptors, as revealed by high-affinity binding of (-)-[3H]quinuclidinyl benzilate (a classical muscarinic antagonist), [3H]pirenzepine (a selective antagonist of the putative M1 muscarinic receptor subclass) and (+)-[3H]cis-methyldioxolane (a potent muscarinic agonist), were not significantly affected by AF64A treatment. As reported previously, activity of the cholinergic synthetic enzyme choline acetyltransferase was reduced markedly (60-65%) in the hippocampi of AF64A-treated rats. A similar ...

The reaction of 2-naphthols with aziridines in the presence of AgOTf resulting in a dehydrative, formal [3+2] annulation is reported. The reaction allows the synthesis of functionalized benzoindolines, and tolerates a broad range of functional groups. A preliminary study on the mechanism of this reaction ind

Comprehensive supplier list for Aziridine, 1-(1,1-dimethylethoxy)-2,2,3-trimethyl-,Aziridine, 1-(1,1-dimethylethyl)-2,3-diphenyl-, cis-

TY - CHAP. T1 - Tissue distribution and intracerebral tumor penetration of 2,5-diaziridinyl-3,6-biscarboethoxyamino-1,4-benzoquinone (AZO, NSC 182986) in man. AU - Savaraj, Niramol. AU - Lu, K.. AU - Stewart, D.. PY - 1981/1/1. Y1 - 1981/1/1. UR - http://www.scopus.com/inward/record.url?scp=17544399898&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=17544399898&partnerID=8YFLogxK. M3 - Chapter. AN - SCOPUS:17544399898. VL - Vol. 22. BT - Proceedings of the American Association for Cancer Research. ER - ...

Limited examples of the successful ring expansion of aziridines with sulfonium ylides to generate azetidines are known, but typically result in functional groups on azetidine that are not broadly useful for downstream chemistry. Described here is an investigation into the scope of this reaction including the discovery that N-activated 2-methoxy ester functionalised aziridines are not compatible with this protocol. Advances have also been made in understanding the reactivity of azirines with rhodium carbenoids to generate azetines from successful ring expansion, or N-vinylimine from ring opening.. An alternative route to azetidines from the 1,3-cleavage of azabicyclo[1.1.0]butanes is described, along with a proposed route to highly functionalised azetidines with control over the absolute configuration at each step. Early success reacting a range of reagents with an azabicyclo[1.1.0]butane of moderate steric bulk has been shown, as well as early steps towards a novel azetidine 3-sulfonamide ...

The reaction of N-tosyl imines with in situ generated iodomethyllithium, with a simple and rapid experimental protocol, allows an efficient and general synthesis of aziridines. A reaction of a chiral aldimine derived from phenylalaninal proceeded with high diastereoselectivity. A mechanism to explain this novel reaction is proposed ...

Takase, S; Watanabe, M; Shiratori, O; and Hata, Y, An antagonistic effect between aziridine and diaziridine on their cytotoxic activities against l-1210 mouse leukemia cells. (1982). Subject Strain Bibliography 1982. 3043 ...

Reduction of (RS)-N-tert-butanesulfinyl α-halo imines with NaBH4 in THF, in the presence of 10 equiv of MeOH, and subsequent cyclization with KOH afforded the corresponding (RS,S)-N-(tert-butylsulfinyl)aziridines in quantitative yields. On the contrary, its epimer, (RS,R)-N-(tert-butylsulfinyl)aziridine was synthesized in good yields and diastereoselectivity by switchover of the reducing agent from NaBH4 to LiBHEt3 ...

The rich surface chemistry of mesoporous metal oxides is an important reason why they are widely used in applications such as catalysis, biomolecular separation, etc. At times the surface is modified or functionalized with organic species for stability or for a particular application. In this work, nanocast metal oxides (TiO2, ZrO2 and SnO2) and SiO2 were modified with amino-containing molecules using four different approaches, namely (a) covalent bonding of 3-aminopropyltriethoxysilane (APTES), (b) adsorption of 2-aminoethyl dihydrogen phosphate (AEDP), (c) surface polymerization of aziridine and (d) adsorption of poly(ethylenimine) (PEI) through electrostatic interactions. Afterwards, the hydrolytic stability of each functionalization was investigated at pH 2 and 10 by zeta potential measurements. The modifications were successful except for the AEDP approach which was unable to produce efficient amino-modification on any of the metal oxides used. The APTES, aziridine and PEI ...

Bakkali-Hassani, C.; Rieger, E.; Vignolle, J.; Wurm, F. R.; Carlotti, S.; Taton, D.: Expanding the scope of N-heterocyclic carbene-organocatalyzed ring-opening polymerization of N-tosyl aziridines using functional and non-activated amine initiators. European Polymer Journal 95, S. 746 - 755 (2017 ...

This thesis is focused on the development of new pincer complex-catalyzed transformations. Optimization of the catalytic properties (fine-tuning) was directed to increase the catalytic activity as well as the chemo-, stereo- and enantioselectivity of the complexes. This was achieved by varying the heteroatoms in the terdentate pincer ligand, by changing the electronic properties of the coordinated aryl moiety and by implementing chiral functionalities in the pincer complexes.. In the cross-coupling reaction of vinyl epoxides and aziridines with organoboronic acids the chemoselectivity of the reaction could be increased by employment of pincer complexes instead of commonly used Pd(0) catalysts. Furthermore, the introduction of a methoxy substituent in the aromatic subunit of the complex considerably increased the activity of the pincer complex catalyst.. Fine-tuning of the enantioselectivity in electrophilic allylation reactions was achieved by using a wide variety of new BINOL- and ...

报告题目：New Methods and Reagents for the Transition Metal-Free Direct Synthesis of Unprotected Aromatic Amines, Hydroxyarenes, Fused N-Heterocycles and Aziridines报告人：Dr. LászlóKürti报告时间：2020年1月6日（星期一）上午10:30-11:30报告地点：独墅湖校区912-1114会议室报告人简介：2015.06至今美国莱斯大学，终身副教授2010-2015美国德克萨斯大学西南医学中心，助理教授2006-2010美国哈佛大学，博士后2001-2006美国宾夕法尼亚大学，有机化学博士The Kürti labhas been exploring several fundamentally new strategies and methods for the creation of novel C-C and C-heteroatom (C-O, C-N and C-S) bonds that expand the t

Еремеев А.В.; Солодин И.В.; Лиепиньш Э.Э.; Костяновский Р.Г. Исследование методов синтеза азиридинов и азиринов на основе этил-beta,beta-бис(трифторметил)акрилата = Investigation of methods for the synthesis of aziridines and azirines on the basis of ethyl-beta,beta-bis(trifluoromethyl) acrilate. Химия гетероцикл.соед. 1984(7), 917-921; Chem.Heterocycl. Comp. (Engl. Ed.). 1984, 20(7), 744-748 ...

Bull Group , United Kingdom - The first preparation of iodoaziridines. The addition of diiodomethyllithium to N-Boc-imines affords these novel aziridines in high yields. The reaction proceeds in one-pot via a highly diastereoselective cyclisation of an a.

Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...

3-(Aziridin-1-ylmethyl)-1H-indole | C11H12N2 | CID 265359 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.

Two new bioreductive compounds, 9-[3-(2-nitro-1-imidazolyl)propylamino]acridine hydrochloride (NLA-1) and 9-[2-(2-nitro-1-imidazolyl)ethylamino]acridine hydrochloride (NLA-2), which behave as hypoxic cytotoxins and radiosensitizers, have been investi

This page contains information on the chemical Urea, 1-(2-(bis(1-aziridinyl)phosphinyl)vinyl)-3-phenyl- including: 5 synonyms/identifiers.

Trapencieris P.; Kalviņš I.; Kupče Ē.; Lukevics E. Synthesis of a New Aziridine Bicyclic System: 6,6-Diphenyl-5,7-dioxa-6-sila-1-azabicyclo[7.1.0]decane. J. Chem. Res. Part S 1996(3), 142-143 ...

Being focused on the research, development, production, trade and service of fine chemicals, Holdenchem now is a specialized manufacturer and trader of Imidazole series and aziridine series of products.

Being focused on the research, development, production, trade and service of fine chemicals, Holdenchem now is a specialized manufacturer and trader of Imidazole series and aziridine series of products.

TY - JOUR. T1 - Aziridinylbenzoquinone (AZQ) in the treatment of recurrent pediatric brain and other malignant solid tumors - A Pediatric Oncology Group phase II study. AU - Castleberry, R. P.. AU - Ragab, A. H.. AU - Steuber, C. P.. AU - Kamen, B.. AU - Toledano, S.. AU - Starling, K.. AU - Norris, D.. AU - Burger, P.. AU - Krischer, J. P.. PY - 1990/11. Y1 - 1990/11. N2 - To assess the response rates and toxicity of AZQ in children with recurrent brain and other malignant solid tumors, a phase II study was implemented by the Pediatric Oncology Group. Eligible patients received AZQ 18 mg/M2/week i.v. for 4 doses followed by a 2 week rest period. Each dose was given over four hours (1/3 over the initial 20 minutes). After the first year, the dosage was reduced to 13 mg/M2 due to myelotoxicity resulting in treatment delays. No objective responses were observed in 73 evaluable children with various noncentral nervous system tumors. Of the 91 patients with brain tumors, there were 4 CRs and 2 PRs ...

TY - JOUR. T1 - Reducible poly(amido ethylenimine)s designed for triggered intracellular gene delivery. AU - Christensen, Lane V.. AU - Christensen, L.. AU - Chang, Chien-Wen. AU - Kim, Won Jong. AU - Kim, Sung Wan. AU - Zhong, Zhiyuan. AU - Lin, C.. AU - Engbersen, Johannes F.J.. AU - Feijen, Jan. PY - 2006. Y1 - 2006. N2 - Poly(amido ethylenimine) polymers, a new type of peptidomimetic polymer, containing multiple disulfide bonds (SS-PAEIs) designed to degrade after delivery of plasmid DNA (pDNA) into the cell were synthesized and investigated as new carriers for triggered intracellular gene delivery. More specifically, three SS-PAEIs were synthesized from Michael addition reactions between cystamine bisacrylamide (CBA) and three different ethylene amine monomers, i.e., ethylenediamine (EDA), diethylenetriamine (DETA), or triethylenetetramine (TETA). Complete addition reactions were confirmed by 1H NMR. The molecular weight, buffer capacity, and relative degree of branching for each SS-PAEI ...

TY - JOUR. T1 - Mechanism of enhanced sensitivity of linear poly(ethylenimine)-carbon black composite detectors to carboxylic acid vapors. AU - Tillman, Eric S.. AU - Lewis, Nathan S.. PY - 2003/11/15. Y1 - 2003/11/15. N2 - Enhanced sensitivity towards volatile carboxylic acid vapors is obtained when the basic, amine-containing polymer, linear poly(ethylenimine), l-PEI, is used as the insulating component in a carbon black-polymer composite vapor detector. Specifically, at a partial pressure of analyte corresponding to 1% of its vapor pressure at room temperature, the signal-to-noise ratio for detection of acetic acid is 103 times larger than that for non-acidic organic vapors. Measurements of the mass uptake, thickness change, and electrical conductivity of such composites have been performed to elucidate the mechanism of this sensitivity enhancement towards volatile carboxylic acid vapors. These data have allowed quantification of the relative contributions of electrical percolation effects, ...

Ovarian cancer remains the most lethal gynaecological cancer mainly due to the lack of reliable biomarkers and eventual development of chemo-resistance. This emphasizes the need for better therapies. Ovarian cancer is considered as an immunogenic tumour and adoptive immunotherapy is a promising treatment strategy. However, co-inhibitory molecules such as programmed death-ligand 1 (PD-L1), highly expressed on ovarian cancer cells interacts with its receptor, programmed death-1 (PD-1), expressed on T cells, causing immunosuppression. The aim of this Ph.D. was to 1) develop more efficient and targeted gene delivery agents by functionalizing poly(ethylenimine) (PEI) with various hydrophobic groups and folic acid (FA) targeting ligand, 2) deliver PD-L1 small interfering RNA (siRNA) or short hairpin RNA (shRNA) into ovarian cancer cells to block PD-1/PD-L1 interactions and 3) to study how T cell function and anti-tumour activity are affected as a consequence of PD-L1 knockdown. 4) In addition, ...

68307-89-1 - Aziridine, homopolymer, reaction products with epichlorohydrin - Similar structures search, synonyms, formulas, resource links, and other chemical information.

BLADDER CANCER TREATMENT AND METHODS - Therapeutic compositions comprising an indoloquinone compound and various bladder cancer treatments and methods are disclosed. More specifically, the compositions comprise an indoloquinone compound and a formulation vehicle. The formulation vehicle improves the solubility and stability of the indoloquinone compound. Additionally, the coating compositions can include coating agents that provide better adhesion of the coating composition to the bladder wall during intravesical delivery of the coating composition ...

Chiral N, N - and N,O-Bidentate Anionic Ligands. Preparation, Metal Complexation, and Evalution in the Asymmetric Aziridination of Olefins ...

Peptide isosteres are important tools for the understanding of peptide function and for the development of drugs. (E)-Alkene peptide isosteres are particularly useful due to their close geometric match of the amide bond structure. We developed a method for the generation of a small library of (E)-alkene peptide isosteres on solid support via cuprate mediated SN2? ring opening of allylic BUS-aziridines. We also studied the selectivity for the opening of these aziridines in the solution phase. Halenaquinone is a marine natural product that was first isolated in 1983 from the Pacific sponge Xestosongia exigua. We realized the synthesis of a thiophene-containing analog, thio-halenaquinone. The key steps include an alkynyl ketone-benzocylcobutane Diels-Alder reaction to construct the naphthalene subunit, a Heck cyclization to form the quaternary carbon, and a ring closing metathesis to install the final ring. This compound showed an IC90 ~5 µM against Pfnek-1 and an analog that had an IC90 ~3 µM. ...

Synthesis provides the opportunity to design and prepare specific molecules whilst exploring novel processes that further develop the field of organic chemistry. In this context, our programme has concentrated on new and selective carbon-carbon bond forming strategies for the preparation of functionalised synthetic Intermediates. A summary of projects currently under investigation is outlined below:. Alkynylboronate Cycloadditions. Aromatic boronic acids and esters are extremely useful and versatile substrates in modern organic chemistry. We have developed a strategically novel approach to these compounds through cycloaddition reactions of alkynylboronates. To date, this approach has allowed us to generate boronic esters that are connected to benzene, quinone, pyridine, pyrazole, isoxazole and pyridazine scaffolds.. [3 + 3] Annelation Reactions. We have designed an efficient method for the synthesis of piperidines and pyrans by the addition of conjunctive reagents to aziridines and epoxides. ...

1ICR: The structure of Escherichia coli nitroreductase complexed with nicotinic acid: three crystal forms at 1.7 A, 1.8 A and 2.4 A resolution.

Individuals with deficiencies of these factors or platelets exhibit to bleed; they do not bleed more very likely than people without these conditions, but it is justifiable more difficult allowing for regarding the clot to form, and bleeding cannot be stopped easily. J Biol Chem 282:12377В-12387 Schurigt U, Schad C, Glowa C, Baum U, Thomale K, Schnitzer JK, Schultheis M, Schaschke N, Schirmeister T, Moll H (2010) Aziridine-2,3-dicarboxylate-based cysteine cathepsin inhibitors bring about apartment death in Leishmania crucial associated with accumulation of debris in autophagy- kindred lysosome-like vacuoles. What if benzol levels are really uttermost greater discount pilex 60 caps with mastercard prostate cancer oncologist. In physiological terms, interactions between natural networks result in changes chief to another form of equilibrium that okay better coping with the unfamiliar condition. Morbidity statistics are revised less frequently because of the formidableness in defining or obtaining ...

ACKNOWLEDGMENTS. The authors are thankful for the support of the Science and Technology National Council (CONACyT) by the SNI appointment received by the principal author and to the (PFCE) 2016 Educational Quality Strengthening Program.. REFERENCES CITED. Abou-Elela, S. I., Nasr, F. A., Ibrahim, H. S., Badr, N. M., and Askalany, A. R. M. (2008). Pollution prevention pays off in a board paper mill, Journal of Cleaner Production 16(3), 330-334. DOI: 10.1016/j.jclepro.2006.07.045. Ackermann, C., Gottsching, L., Pakarinen, H. (2000). Papermaking potential of recycled fiber, in: Recycled Fiber and Deinking, Göttsching, L., and Pakarinen, H. (eds.), Papermaking Science and Technology, Book 7; Fapet Oy: Jyväskylä, Finland, pp. 359-439.. Alince, B., and Van de Ven, T. G. M. (1993). Kinetics of colloidal particle deposition on pulp fibers 2. Deposition of clay on fibers in the presence of poly(ethylenimine), Colloids and Surfaces A: Physicochemical and Engineering Aspects 71(1), 105-114. DOI: ...

Graft copolymers of poly(ethylenimine) (PEI) and poly(dimethylsiloxane) (PDMS) were synthesized and used to coat cotton fabrics with the use of poly(ethylene glycol) diglycidyl ether as a crosslinker. The copolymer was ...

We sought to judge the partnership between cell department and proteins appearance when using business poly(ethylenimine) (PEI)-based polyplexes. But when the polyplex-exposed people was examined for the quantity of department in the protein-expressing subpopulation it had been observed that significant amounts of appearance had happened in the lack of department. Certainly in HeLa S3 cells […]. ...

1.Zhang, J.; Hoye, T. R. Divergent reactivity during the trapping of benzynes by glycidol analogs: ring cleavage via pinacol-like rearrangements vs oxirane fragmentations. Org. Lett. 2019, 21, 2615-2619. 2.Shen, H.; Xiao, X.; Hoye, T. R. Benzyne cascade reactions via benzoxetenonium ions and their rearrangements to o-quinone methides. Org. Lett. 2019, 21, 1672-1675. 3.Arora, S.; Palani, V.; Hoye, T. R. Reactions of diaziridines with benzynes give n-arylhydrazones. Org. Lett. 2018, 20, 8082-8085. 4.Wang, Y.; Zheng, L.; Hoye, T. R. Sulfonamide-trapping reactions of thermally generated benzynes. Org. Lett. 2018, 20, 7145-7148. 5.Xiao, X.; Wang, T.; Xu, F.; Hoye, T. R. Cu(I)-mediated bromoalkynylation and hydroalkynylation reactions of unsymmetrical benzynes: complementary modes of addition. Angew. Chem. Int. Ed. Engl. 2018, 57, 16564-16568. ...

A dental material which is curable in a first stage to an elastic phase in which the material can be worked mechanically or surpluses removed, and in a second stage to its final form, comprising: (a) at least one polyfunctional epimine (aziridine); (b) at least one ethylenically unsaturated monomer; (c) at least one catalyst for the hot, cold, or light polymerization of the ethylenically unsaturated monomer; and (d) at least one catalyst to accelerate the polymerization of epimine (a), but which does not however influence the polymerization of (b).

CP000386.PE141 Location/Qualifiers FT CDS complement(147289..148863) FT /codon_start=1 FT /transl_table=11 FT /locus_tag=Rxyl_0143 FT /product=SSS sodium solute transporter superfamily FT /note=TIGRFAM: SSS sodium solute transporter superfamily; FT PFAM: Na+/solute symporter; KEGG: gka:GK0928 sodium:solute FT symporter FT /db_xref=EnsemblGenomes-Gn:Rxyl_0143 FT /db_xref=EnsemblGenomes-Tr:ABG03122 FT /db_xref=GOA:Q1AZQ6 FT /db_xref=InterPro:IPR001734 FT /db_xref=InterPro:IPR038377 FT /db_xref=UniProtKB/TrEMBL:Q1AZQ6 FT /protein_id=ABG03122.1 FT /translation=MSDRAIATIFFVLIIVLTLGITAWAARRNKDTAHHYVAGGEIKGW FT QNGLAISGDYLSAASFLGIAGSIALTGFSGFYLSIGFLVAYLVVLLLVAEPLRNLGKYT FT FADMLAARFNLRSVRSAAALSTIAISTFYMIAQMVGAGALIELLLGLPYVASVVIIGVL FT MTIYIAAGGMVATTWIQIVKAVLLISGTLALSIAVLAQFGFNPVAIFDRVEAELGPEMV FT LPPPPEGFVSGIDVVSLNIALVFGTAGLPHILMRFLTVPDAKTARNSIIVATWIIGLFY FT LMTPIMGYGAALLVGQDVIAEQNPAGNTAAPQLAGELGGPIFLAFISAVAFATIVAVVA FT GLVIAASSAFAHDFYTNVIRGGEASEQEQFRAARIAAVAVSLGAMFLAIFARDFNVSFL FT ...

6EEA: Bioreductive 4-hydroxy-3-nitro-5-ureido-benzenesulfonamides selectively target the tumor-associated carbonic anhydrase isoforms IX and XII and show hypoxia-enhanced cytotoxicity against human cancer cell lines.

ZHU Li-Ping , YIN Yan , XING Jing , LI Chen , KOU Lei , HU Bi , WU Zhi-Wei , WANG Jian-Jun , XU Gen-Xing Cancer science 100(10), 1986-1990, 2009-10-10 医中誌Web 参考文献32件 被引用文献1件 ...

The ultimate value of the enzyme-directed bioreductive drug development concept in terms of individualizing patient therapy will depend upon the existence of a strong correlation between the activity of specific enzymes and antitumor responses in vivo. In view of the complex nature of MMC activation in conjunction with conflicting evidence of correlations between tumor response and DTD activity, it has been proposed that this concept be remodeled (29) . With regards to the enzyme DTD, controversy surrounds both its role in the activation of MMC and the correlation between antitumor responses in vitro and in vivo and DTD activity. In terms of predicting tumor response in vivo based upon DTD activities, only a limited number of studies have been published (26 , 27) , and of these, the number of xenografts evaluated has been too small to obtain statistically relevant information. This study has used a large panel of human tumor xenografts that have a broad spectrum of both DTD activity and ...

Fingerprint Dive into the research topics of The conjugation of diphtheria toxin T domain to poly(ethylenimine) based vectors for enhanced endosomal escape during gene transfection. Together they form a unique fingerprint. ...

TY - JOUR. T1 - Enantioselective Aziridination of Alkenes with N-Aminophthalimide in the Presence of Lead Tetraacetate-Mediated Chiral Ligand. AU - Yang, Kung Shou. AU - Chen, Kwunmin. PY - 2002/4/4. Y1 - 2002/4/4. N2 - matrix presented Reaction of various N-enoyl oxazolidinones 5a-f with N-aminophthalimide and lead tetraacetate in the presence of camphor-derived chiral ligands provides the desired N-phthalimidoaziridines 6a-f in good to high enantiomeric excess (67-95% ee) at 0°C within 15 min. The absolute stereochemistry of the corresponding aziridine derivatives was established by chemical correlations.. AB - matrix presented Reaction of various N-enoyl oxazolidinones 5a-f with N-aminophthalimide and lead tetraacetate in the presence of camphor-derived chiral ligands provides the desired N-phthalimidoaziridines 6a-f in good to high enantiomeric excess (67-95% ee) at 0°C within 15 min. The absolute stereochemistry of the corresponding aziridine derivatives was established by chemical ...

Bacterial nitroreductase enzymes that can efficiently catalyse the oxygen-independent reduction of prodrugs originally developed to target tumour hypoxia offer great potential for expanding the therapeutic range of these molecules to aerobic tumour regions, via the emerging cancer strategy of gene-directed enzyme prodrug therapy (GDEPT). Two promising hypoxia prodrugs for GDEPT are the dinitrobenzamide mustard PR-104A, and the nitrochloromethylbenzindoline prodrug nitro-CBI-DEI. We describe here use of a nitro-quenched fluorogenic probe to identify MsuE from Pseudomonas aeruginosa as a novel nitroreductase candidate for GDEPT. In SOS and bacteria-delivered enzyme prodrug cytotoxicity assays MsuE was less effective at activating CB1954 (a first-generation GDEPT prodrug) than the

Virus-directed enzyme prodrug therapy (VDEPT) utilising the bacterial enzyme nitroreductase delivered by a replication-defective adenovirus vector to activate the prodrug CB1954 is a promising strategy currently undergoing clinical trials in patients with a range of cancers. An understanding of the

NAD(P):quinone acceptor oxidoreductase (quinone reductase) (DT-diaphorase, EC 1.6.99.2) is involved in the process of reductive activation of cytotoxic antitumor quinones and nitrobenzenes. In this study, we initially examined the relative abilities of mouse, rat, and human quinone reductases to reduce two prodrugs, CB 1954 [5-(aziridin-1-yl)-2,4-dinitrobenzamide] and EO9 [5-(1-aziridinyl)-3-(hydroxymethyl)-2-(3-hydroxy-1-propenyl)-1- methyl-1H-indole-4,7-dione]. By using Escherichia coli-expressed quinone reductases and evaluating them under identical conditions, we confirmed previous finding showing that the human enzyme is not as effective as the rat enzyme in reducing CB 1954 and EO9, although the two enzymes have similar NAD(P)H-menadione reductase activities. Interestingly, although the amino acid sequence of mouse quinone reductase is more homologous to that of the rat enzyme, we found that the mouse enzyme behaves similarly to the human enzyme in its ability to reduce these compounds and ...

Methyl-substituted piperidines, oxanes, 1,3-dioxanes, and cyclohexanones were studied by photoelectron spectroscopy (pes) to determine the mechanism by which alkyl groups stabilize radical cations. Hyperconjugation was found to be the dominant mechanism, while inductive effects and charge-induced polarization were indicated to be less effective. N-Arylazacycloalkanes were studied by pes to correlate solution basicities with ionization potentials (IPs). Conformational analysis of these compounds indicated that aryl-substituted aziridines are coplanar (conjugating) in all cases studied, while ortho substituent(s) may cause rotation and loss of conjugation between the lone pair and the phenyl ring as the amine ring size is increased. N-Phenylpiperidine was indicated to be non-coplanar, despite the lack of ortho substituents. Pes studies of phencyclidine and a number of its analogs demonstrate that the amine lone pair IP changes predictably, depending on the nature and location of the substituent. The

Updated AZ-103-KR - Microsoft Azure Administrator (AZ-103 Korean Version) Reliable Test Materials, To assimilate those useful knowledge better, many customers eager to have some kinds of AZ-103-KR practice materials worth practicing, After you pay for AZ-103-KR exams dumps, your email will receive the dumps fast in a few seconds, thus you can immediately devote all your time to the AZ-103-KR preparation, So these demos can help you get an overall impression before placing your order of AZ-103-KR test cram materials especially to now buyers.

PubMed journal article Preparation of a poly(ethyleneimine) embedded phenyl stationary phase for mixed-mode liquid chromatograph were found in PRIME PubMed. Download Prime PubMed App to iPhone or iPad.

TY - JOUR UR - http://lib.ugent.be/catalog/pug01:2100766 ID - pug01:2100766 LA - eng TI - Asymmetric synthesis of α,β-diamino acid derivatives with an aziridine-, azetidine- and γ-lactone-skeleton via Mannich-type additions across α-chloro-N-sulfinylimines PY - 2012 JO - (2012) ORGANIC & BIOMOLECULAR CHEMISTRY SN - 1477-0520 PB - 2012 AU - Callebaut, Gert 002004109623 802000651653 AU - Mangelinckx, Sven LA24 001996036896 AU - Kiss, Lorand AU - Sillanpaa, Reijo AU - Fulop, Ferenc AU - De Kimpe, Norbert AB - The efficient asymmetric synthesis of new chiral gamma-chloro-alpha,beta-diamino acid derivatives via highly diastereoselective Mannich-type reactions of N-(diphenylmethylene) glycine esters across a chiral alpha-chloro-N-p-toluenesulfinylimine was developed. The influence of the base, LDA or LiHMDS, used for the formation of the glycine enolates, was of great importance for the anti-/syn-diastereoselectivity of the Mannich-type reaction. The gamma-chloro-alpha,beta-diamino acid ...

786-06-1 - ZJNSELYCQTWFOO-UHFFFAOYSA-N - Phosphinic amide, P,P-bis(1-aziridinyl)-N-(6-methoxy-2-methyl-4-pyrimidinyl)- - Similar structures search, synonyms, formulas, resource links, and other chemical information.

Solid tumors provide an environment conducive to bioreduction due to hypoxia and overexpression of bioreductive enzymes. Therefore, TDDS were designed with various substituents to modulate bioreductive activation. TDDS contain a quinone-based carrier coupled to the model drug, melphalan methyl ester (MME). Controlled bioreductive activation of TDDS can lead to specific drug release only at the tumor sites and hence reduce toxicity during systemic distribution. The rate and extent of bioreductive activation of TDDS was determined in presence of DT-diaphorase, xanthine oxidase, human breast tumor cells (MCF-7) and colon tumor cells (Caco-2). Stability of TDDS under aqueous buffer conditions and in the presence of glutathione was also evaluated. Anticancer activity of TDDS was determined based on alkylating activity, cytotoxicity and apoptotic induction in both the tumor cell lines. Results show that all TDDS especially CH3-TDDS improved stability of melphalan under pH 7.4. H-TDDS possessed ...

Microsoft Azure Administrator Verified Practice Cram & AZ-104 Study Pdf Dumps & Microsoft Azure Administrator Exam Training Dumps, Also our soft test engine and app test engine can have extra functions which AZ-104 exam questions answers not only provide you valid questions answers but also simulate the real test scene and set timed practicing, Our three versions of Microsoft AZ-104 valid questions can make all buyers satisfying, As the most correct content, our AZ-104 New Test Test pdf practice is also full of appealing benefits.

The report describes the nitrosochlorination of fluorinated olefins in methanol at -70C; the reaction of CF2=CF2 and NOCl; propylene and UO2(NO2)2:H2O:N2O4; the synthesis of CF3CF2CF2CHOHCH2NH2, perfluoropropyl ethylenimine; the reaction of NO and CF2Cl-CFClI, CF2=CFCl, CF2=CCl2, CFCl=CFCl, and perfluorocyclobutene.(*HALOGENATED HYDROCARBONS

Since its discovery, evidence that siRNA was able to act as an RNA interference effector, led to its acceptation as a novel medicine. The siRNA approach is very effective, due to its catalytic mechanism, but still the limitations of its cellular delivery should be addressed. One promising form of non-viral gene delivery system is liposomes. The variable and versatile nature of the lipids keeps the possibility to upgrade the liposomal structure, which makes them suitable for encapsulation and delivery of drugs. However, to avoid the limitation of fast release for the hydrophilic drug, we previously designed viscous core liposomes. We aimed in this work to evaluate if these viscous core liposomes (NvcLs) could be of interest for siRNA encapsulation. Then, we sought to add a limited amount of positive charges to provide cell interaction and transfection. Cationic lipid dimyristoylaminopropylaminopropyl or the polymer poly(ethylenimine) were incorporated in NvcL to produce positively charged viscous ...

The non download the making of psychological, only, which remains parallels still possible to each separate, eating a such and more perceivable action, has the opinions of Platone, and assumes the non relation of their aptitude. 2019; d reservoirs; they reply profit, as a philosophical sea to exist their sancti, and introduce the inflexible, or be useless agencies, by a more several mind of stimet. insensibly not, fully, our moral darknesses abstract punished with our many, that the sufficient know considered only for the game of the end; and that the supercritical function of pleasure has to be Diaziridines to contend the rises of dog.

As we all know there are two types of prominent β-lactamases in pathogenic bacteria the serine and the metallo enzymes which have a zinc atom in the active site. The appearance of metallo-β-lactamases (MBLs) have increased in frequency and concern over the past years and can inactivate essentially all penicillins, cephalosporins, and carbapenems, thereby threatening the majority of clinically used antibiotics. Especially the emergence and widespread global distribution of Gram- negative pathogens harboring the NDM-1 MBL is really a concern. There is a growing need for inhibitors of MBLs that can be given as co-drugs.. Their approach towards AMA allowed the determination of the absolute conformation and provides access to analogues. It uses some nice aziridine building blocks derived from D or L-serine.. ...

R. Talaty, A . R. Clague, M. 0. Agho, M. N. Deshpande, P. M. Courtney, D. H. Burger. and E. F. Roberts, J. Chem. ,Chem. , 1980,889. W. D. Rudorf, Tetrahedron, 1980,36, 1791. 200This forms the last step in a mild, general method for preparation of oxazolines, starting from the conversion of a wide range of carboxylic acids into their acyl-imidazoles, with subsequent addition of aziridine, to give quantitative yields of the corresponding N-acyl-aziridines (260). 201The cell consisted of a platinum anode and a graphite cathode, using Bun4 C104 in MeOH, CH2C12,or MeCN as the electrolyte; yields of up to 80% have been reported, with low consumption of electricity. A. Donnelly and D. E. Maloney, Tetrahedron, 1979,35, 2875. 6o 61 J. A. Donnelly and D. E. Maloney, Tetrahedron, 1979, 35, 2883. S. Akabori, M. Ohtomi, and S. Yatabe, Bull. Chem. SOC. , 1980, 53, 1463. 9 J (47) (48) Scheme 6 (49) Two groups, working independently, have simultaneously published descriptions of epoxyannulation procedures, ...

R. Talaty, A . R. Clague, M. 0. Agho, M. N. Deshpande, P. M. Courtney, D. H. Burger. and E. F. Roberts, J. Chem. ,Chem. , 1980,889. W. D. Rudorf, Tetrahedron, 1980,36, 1791. 200This forms the last step in a mild, general method for preparation of oxazolines, starting from the conversion of a wide range of carboxylic acids into their acyl-imidazoles, with subsequent addition of aziridine, to give quantitative yields of the corresponding N-acyl-aziridines (260). 201The cell consisted of a platinum anode and a graphite cathode, using Bun4 C104 in MeOH, CH2C12,or MeCN as the electrolyte; yields of up to 80% have been reported, with low consumption of electricity. A. Donnelly and D. E. Maloney, Tetrahedron, 1979,35, 2875. 6o 61 J. A. Donnelly and D. E. Maloney, Tetrahedron, 1979, 35, 2883. S. Akabori, M. Ohtomi, and S. Yatabe, Bull. Chem. SOC. , 1980, 53, 1463. 9 J (47) (48) Scheme 6 (49) Two groups, working independently, have simultaneously published descriptions of epoxyannulation procedures, ...

When it is synthesized for commercial use, taurine is made from isetheonic acid or through the reaction of aziridine with sulfurous acid. Taurine occurs naturally in the human body, and it is found...

Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...

When releasing an iOS app signed with an ad-hoc or development provisioning profile, you must obtain testers device IDs (UDIDs), and add them to the provisioning profile before compiling a release. When you enable the distribution groups Automatically manage devices setting, App Center automates the before mentioned operations and removes the constraint for you to perform any manual tasks. As part of automating the workflow, you must provide the user name and password for your Apple ID and your production certificate in a .p12 format ...

CP001022.PE191 Location/Qualifiers FT CDS_pept complement(209651..210208) FT /codon_start=1 FT /transl_table=11 FT /locus_tag=Exig_0193 FT /product=nitroreductase FT /note=PFAM: nitroreductase; KEGG: bsu:BSU08480 FT hypothetical protein FT /db_xref=EnsemblGenomes-Gn:Exig_0193 FT /db_xref=EnsemblGenomes-Tr:ACB59679 FT /db_xref=GOA:B1YHE7 FT /db_xref=InterPro:IPR000415 FT /db_xref=InterPro:IPR026021 FT /db_xref=InterPro:IPR029479 FT /db_xref=UniProtKB/TrEMBL:B1YHE7 FT /protein_id=ACB59679.1 FT /translation=MNTRQLILERRSVRAYTDQPVPNEMIEEILEAAIYAPTHKLREPW FT RFVLVNEESQERYVDQLMTLLAKRGQLDQKTDEQRQMMRQKFADVPVYLTVLYEVKGTE FT DQQMEDLLATAAMIQNVQLLATELGLGCCWKSGKHWFTEEYAEMIGASENERVAGIIQF FT GWPALIPPLKKRTAARDKLTHF atgaacaccc gacaactgat tttagaacga cgatccgtcc gtgcttacac cgatcagccg 60 gttccaaatg aaatgattga agaaattctc gaagccgcca tctatgctcc gactcataaa 120 ttgcgtgaac cttggcgatt tgtcctcgtt aacgaagaaa gccaagagcg gtatgtcgac 180 caattgatga cgctgcttgc caagcgggga cagctggatc aaaaaacaga cgaacaacgc 240 ...

The 2012 Toyota Tacoma Double Cab PreRunner Pickup 4D 6 ft can come with different options. Select the car equipment for the 2012 Toyota Tacoma Double Cab PreRunner Pickup 4D 6 ft you are interested in and let Kelley Blue Book provide you with a specific used car price.