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 - ...
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 ...
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.
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.
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 - 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: ...
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 ...
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
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 ...
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 ...
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
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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.. ...