Congener of CYTARABINE that is metabolized to cytarabine and thereby maintains a more constant antineoplastic action.
A compound that, on administration, must undergo chemical conversion by metabolic processes before becoming the pharmacologically active drug for which it is a prodrug.
Exclusive legal rights or privileges applied to inventions, plants, etc.
The process of finding chemicals for potential therapeutic use.
The spectrum of different living organisms inhabiting a particular region, habitat, or biotope.
Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
Chemistry dealing with the composition and preparation of agents having PHARMACOLOGIC ACTIONS or diagnostic use.
A plasma alpha 2 glycoprotein that accounts for the major antithrombin activity of normal plasma and also inhibits several other enzymes. It is a member of the serpin superfamily.
An absence or reduced level of Antithrombin III leading to an increased risk for thrombosis.
Endogenous factors and drugs that directly inhibit the action of THROMBIN, usually by blocking its enzymatic activity. They are distinguished from INDIRECT THROMBIN INHIBITORS, such as HEPARIN, which act by enhancing the inhibitory effects of antithrombins.
An endogenous family of proteins belonging to the serpin superfamily that neutralizes the action of thrombin. Six naturally occurring antithrombins have been identified and are designated by Roman numerals I to VI. Of these, Antithrombin I (see FIBRIN) and ANTITHROMBIN III appear to be of major importance.
Activated form of factor X that participates in both the intrinsic and extrinsic pathways of blood coagulation. It catalyzes the conversion of prothrombin to thrombin in conjunction with other cofactors.
Manner or style of walking.
A highly acidic mucopolysaccharide formed of equal parts of sulfated D-glucosamine and D-glucuronic acid with sulfaminic bridges. The molecular weight ranges from six to twenty thousand. Heparin occurs in and is obtained from liver, lung, mast cells, etc., of vertebrates. Its function is unknown, but it is used to prevent blood clotting in vivo and vitro, in the form of many different salts.
That region of the immunoglobulin molecule that varies in its amino acid sequence and composition, and comprises the binding site for a specific antigen. It is located at the N-terminus of the Fab fragment of the immunoglobulin. It includes hypervariable regions (COMPLEMENTARITY DETERMINING REGIONS) and framework regions.
The misinterpretation of a real external, sensory experience.
Polypeptide chains, consisting of 211 to 217 amino acid residues and having a molecular weight of approximately 22 kDa. There are two major types of light chains, kappa and lambda. Two Ig light chains and two Ig heavy chains (IMMUNOGLOBULIN HEAVY CHAINS) make one immunoglobulin molecule.
The largest of polypeptide chains comprising immunoglobulins. They contain 450 to 600 amino acid residues per chain, and have molecular weights of 51-72 kDa.
Partial immunoglobulin molecules resulting from selective cleavage by proteolytic enzymes or generated through PROTEIN ENGINEERING techniques.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.

Effects of 2,2'-O-cyclocytidine and acyclovir on latent herpes simplex virus in trigeminal ganglia of mice. (1/4)

The effects of 2,2'-O-cyclocytidine (CC) and acyclovir (ACV) on latent herpes simplex virus (HSV) in trigeminal ganglia were studied in an in vitro model using reactivation of HSV type 1 (HSV-1) as a model. It was shown that both CC (10 micrograms/ml) and ACV (2.5 micrograms/ml) significantly inhibited the reactivation of the latent HSV-1 in infected ganglia. The effect of CC (25 micrograms/ml), which was as good as that of ACV (10 micrograms/ml), did not last as long as that of ACV after removal of the drugs. The latent state of HSV-1 in vitro was dependent on the continuous presence of either drug. Even though the latent HSV-1 could not be eliminated completely from the trigeminal ganglia by discontinuous administration of either drug, its titers were markedly reduced. The combination of CC and ACV had a synergistic effect on preventing the reactivation of the latent HSV-1 in vitro.  (+info)

Antiviral activities of acyl derivatives of 2,2'-anhydro-1-beta-D-arabinofuranosylcytosine and 1-beta-D-arabinofuranosylcytosine in cell culture. (2/4)

Antiviral activities of acyl derivatives (3'-O-octanoyl and 3'-O-decanoyl) of 2,2'-anhydro-1-beta-d-arabinofuranosylcytosine (cyclo-C) and 1-beta-d-arabinofuranosylcytosine (Ara-C) were compared with other antiviral nucleosides, and some biological characteristics of the antiviral activity were investigated. Among those synthesized acyl derivatives, 3'-O-decanoyl ara-C was the most active against deoxyribonucleic acid viruses, with an activity comparable to that of Ara-C. Acyl derivatives of cyclo-C were somewhat less active than their Ara-C counterparts. In the value of therapeutic index, 1-beta-d-arabinofuranosyladenine was superior to the others, followed by 5-iodo-2'-deoxyuridine. In comparing the sensitivity of two serotypes of herpes simplex virus it was found that Ara-C and its ester, as well as its cyclo-C counterpart, were more active against the type 2 than the type 1 strain. The activity of 3'-O-decanoyl Ara-C, like that of its parent, was diminished by treatment with cytidine deaminase from mouse kidney, but 3'-O-decanoyl cyclo-C was resistant to this treatment. In comparative studies of 3'- and 5'-O-acyl Ara-C's, antivaccinia virus activity of 3'-O-palmitoyl Ara-C was significantly superior to its 5'-counterpart. The inhibitory activity of 5'-O-decanoyl Ara-C was markedly reduced by the presence of a threefold molar excess of eserine sulfate, a choline esterase inhibitor, whereas the 3'-acyl Ara-C was not affected by the inhibitor in any combination. This result indicates that enzymatic hydrolysis of the 3'-ester to Ara-C, which is inhibited by eserine sulfate, did not occur in this cell culture.  (+info)

Synergistic effects of the combination of cis-platinum diamminodichloride and 2,2'-anhydro-1-beta-D-arabinofuranosyl-5-fluorocytosine in transplanted mouse leukemias. (3/4)

cis-Platinum diamminodichloride has been studied in combination with 2,2'-anhydro-1-beta-D-arabinofuranosyl-5-fluorocytosine on an every-4-day schedule in various lines of mouse leukemia. This combination is synergistic in leukemias L1210 and P388 and sublines made resistant to 5-fluorouracil or methotrexate. There is no cross-resistance between cis-platinum diamminodichloride and 2,2'-anhydro-1-beta-D-arabinofuranosyl-5-fluorocytosine, but the combination is no more effective against lines of leukemia made resistant to cis-platinum diamminodichloride or to 2,2'-anhydro-1-beta-D-arabinofuranosyl-5-fluorocytosine than either single active compound alone. Since these compounds have no cross-resistance, act by quite different mechanisms of action, and have different limiting toxicity, the combination is now being evaluated clinically.  (+info)

Tyramine-like effect of cyclocytidine (2,2'-anhydro-1-beta-arabinofuranosylcytosine hydrochloride), an antineoplastic agent. (4/4)

Since cyclocytidine (2,2'-anhydro-1-beta-arabinofuranosylcytosine hydrochloride) was introduced as an antineoplastic agent for the treatment of lymphatic leukemia, sinus acceleration and an increase in systemic blood pressure has been reported as its systemic effects in the clinical cases. These cardiovascular effects of cyclocytidine were observed also in anesthetized dogs, but not in reserpine-pretreated animals. Increases in heart rate and in systemic blood pressure were prevented by propranolol and phentolamine, respectively. The mechanism of these sympathomimetic effects was further analysed in the excised, blood-perfused canine sinoatrial node and papillary muscle preparations with a support dog. Positive chronotropic and inotropic responses to cyclocytidine were abolished by desipramine, propanolol, and pretreatment with reserpine but not by tetrodotoxin and hexamethonium. The tyramine-like actions of cyclocytidine at adrenergic neuronal terminals were discussed in conjunction with the uptake mechanism of the drug into the tumor cells.  (+info)

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BH-AC-AMP protocol: chemotherapy protocol consisting of N(4)-behenoyl-1-beta-arabinofuranosylcytosine, aclarubicin, 6-mercaptopurine & prednisolone
Classifying the isomeric 4-amino-cyclohexane-carboxylic acids and their acyl derivatives in the cis- or trans series is certain thanks to the investigations of J Houben and A Pfau, Ber dtsch chem Ges 49 2294 (1916), L Orthner and R Hein (Biochem Z 262 461 (1933), G Wendt (Chem Ber 75 425 (1942) and E Ferber and H Br ckner (Chem Ber 76 1019 (1943).. As the acid saponification in mild conditions of the ethyl ester prepared from the amino acids and their hydrochlorides returned to the respective starting product only, the steric classification can be considered valid for the ethyl esters too.. Spectroscopic investigation of the constitution of the amides prepared confirmed their constitution. Comparison of the IR photos of cis-cis-IV, trans-trans-IV and cis-trans-IV as well as cis-VI and trans-VI shows that the compounds in the cis- and trans-series have the same configuration.. The differing steric alignment of the COOC2H5 group in the cis- and trans-forms is evident from the homogenous shifts in ...
TY - JOUR. T1 - Synthesis of acyl derivatives of salicin, salirepin, and arbutin. AU - Stepanova, Elena Vledimirovna. AU - Belyanin, Maxim L.. AU - Filimonov, Victor D.. PY - 2014/3/31. Y1 - 2014/3/31. N2 - The total synthesis of two natural phenolglycosides of the family Salicaceae, namely: populoside and 2-(β-d-glucopyranosyloxy)-5-hydroxy benzyl (3-methoxy-4-hydroxy) cinnamoate and nine not found yet in plants acyl derivatives of phenoglycosides: 2-(β-d-glucopyranosyloxy)-benzylcinnamoate, 2-(β-d-glucopyranosyloxy)-benzyl (4-hydroxy) benzoate, 2-(β-d-glucopyranosyloxy)-benzyl (3-methoxy-4-hydroxy) benzoate, 2-(β-d-glucopyranosyloxy)-5-hydroxy benzyl (3,4-dihydroxy) cinnamoate, 2-(β-d-glucopyranosyloxy)-5-hydroxy benzylcinnamoate, 2-(β-d- glucopyranosyloxy)-5-hydroxy benzyl (4-hydroxy) benzoate, 2-(β-d- glucopyranosyloxy)-5-hydroxy benzyl (3-methoxy-4-hydroxy) benzoate, 2-(β-d-glucopyranosyloxy)-5-benzoyloxy benzylbenzoate and 4-(β-d-glucopyranosyloxy)-phenylbenzoate, starting from ...
The Importance of Carboxylic Acids (RCO2H). Starting materials for acyl derivatives (esters, amides, and acid chlorides)Abundant in nature from oxidation of aldehydes and alcohols in metabolismAcetic acid, CH3CO2H, - vinegarButanoic acid, CH3CH2CH2CO2H (rancid butter) Long-chain aliphatic acids...
CISPLATIN Kemasan : vial 10 mg/20 cc, 25 mg/50 cc Cara melarutkan: Setiap 1 mg cis-platinum dilarutkan dengan 1 cc aquabidest. Dosis : 100 mg/m2 Premedikasi : inj Ondansentron 0,1 - 0,2 mg/kgBB/ 6-12 jam Cara pemberian : Jalur 1 : lakukan hidrasi dengan larutan 2A 250cc selama 6 - 8 jam -|…
Gibson, M H. and Bertalanffy, F D., In vivo synchrony of solid b16 melanoma by 1-beta-d-arabinofuranosyl- -cytosine (ara-c). Abstr. (1971). Subject Strain Bibliography 1971. 68 ...
So there I was, puffing and dreaming about the finish point when, out of the corner of my eye, a green-helmeted about nine year old boy appeared riding a slender, jet-black bmx. At first, I thought he would whiz uneventfully by or, at most, stick out his hand for a passing high-five which is the customary practice of some of the other kids of the area. This kid was far more ambitious ...
B-Specific) Enoyl-(Acyl-Carrier Protein) Reductase (NADPH: An enzyme that catalyzes the oxidation of acyl-[acyl-carrier protein] to trans-2,3-dehydroacyl-[acyl-carrier protein] in the fatty acid biosynthesis pathway. It has a preference for acyl derivatives with carbon chain length from 4 to 16.
2 For my friends. Aware of how they worry about me and of how terrible I am when it comes to staying in touch, I want them to know that I still feel them lifting me up ...
The use of a prodrug, a conjugate of an active drug with a lipophilic substituent, is a good way of increasing the cutaneous absorption of a drug. However, the activity of dermal hydrolases has rarely been investigated in humans, or experimental animals. In the present study, we focused on the identification of rat dermal esterases and the hydrolysis of a prodrug during permeation across rat skin. We found that carboxylesterase (CES), especially the rat CES1 isozyme, Hydrolase A, is expressed in rat skin and that the hydrolysis of p-nitrophenyl acyl derivatives and caproyl-propranolol (PL) was 20-fold lower in the 9000g supernatant fraction of skin homogenate than in liver microsomes. A permeation study of caproyl-PL was performed in rat full-thickness and stripped skin using a flow-through diffusion cell. Caproyl-PL was easily partitioned into the stratum corneum and retained, not only in the stratum corneum, but also in viable epidermis and dermis. Caproyl-PL could barely be detected in the receptor
... ancitabine (INN) Ancobon Ancotyl ancriviroc (USAN) ancrod (INN) andolast (INN) Andriol Androcur Androderm Androgel Android-f ...
... ancitabine MeSH D13.570.065.950 - vidarabine MeSH D13.570.230.229 - deoxyadenosines MeSH D13.570.230.229.075 - cladribine MeSH ... ancitabine MeSH D13.570.685.245.500 - deoxycytidine MeSH D13.570.685.245.500.250 - bromodeoxycytidine MeSH D13.570.685.245. ...
Ancitabine. 20.00. 0.139. 0.2005. −2.418. −2.62. 3.20. 225.21. Delaviridine. 6.67. 0.034. 0.0014. −2.3428. 2.77. 0.086. 456.57 ...
Ancitabine. Congener of CYTARABINE that is metabolized to cytarabine and thereby maintains a more constant antineoplastic ...
... pyrimidine analogs such as ancitabine, azacitidine, 6-azauridine, carmofur, cytarabine, dideoxyuridine, doxifluridine, ...
... pyrimidine analogs such as ancitabine, azacitidine, 6-azauridine, carmofur, cytarabine, dideoxyuridine, doxifluridine, ...
... ancitabine hydrochloride, enocitabine, azaserine and diazomycin; antibiotics such as actinomycin D, cyclomycin, mitomycin C, ...
Pyrimidine Analogs -Ancitabine, Azacitidine, 6-Azauridine, Carmofur, Cytarabine, Doxifluridine, Enocitabine, Floxuridine, ...
... pyrimidine analogs such as ancitabine, azacitidine, 6-azauridine, carmofur, cytarabine, dideoxyuridine, doxifluridine, ...
... analogs such as ancitabine, azacitidine, 6-azauridine, carmofur, cytarabine, dideoxyuridine, doxifluridine, enocitabine, ...
Antitumor agents such as, 5-fluorouracil and derivatives thereof, krestin, picibanil, ancitabine, cytarabine and the like; 26. ...
... ancitabine (INN) Ancobon Ancotyl ancriviroc (USAN) ancrod (INN) andolast (INN) Andriol Androcur Androderm Androgel Android-f ...
... ancitabine MeSH D13.570.065.950 - vidarabine MeSH D13.570.230.229 - deoxyadenosines MeSH D13.570.230.229.075 - cladribine MeSH ... ancitabine MeSH D13.570.685.245.500 - deoxycytidine MeSH D13.570.685.245.500.250 - bromodeoxycytidine MeSH D13.570.685.245. ...
... ancitabine, ancrod, andolast, androstanolone, angiotensinamide, angiotensine ii, anidoxime, anilamate, aniléridine, anilopam, ... ancitabine, ancrod, andolast, androstanolone, angiotensin ii, angiotensinamide, anidoxime, anilamate, anileridine, anilopam, ... ancitabine, ancriviroc, ancrod, andolast, androstanolone, anécortave, angiotensinamide, angiotensine ii humaine, anidoxime, ... ancitabine, ancriviroc, ancrod, andolast, androstanolone, anecortave, angiotensin ii, angiotensinamide, anidoxime, ...
... ancitabine, androstanediol, androstanol propionate, androstenetrione, androstenonol propionate, anethole, anguidine, anidoxime ...
ancitabine hydrochloride. The hydrochloride salt of a cytarabine congener prodrug with antineoplastic activity. Upon ... Compared to cytarabine, a more prolonged, consistent cytarabine-mediated therapeutic effect may be achieved with ancitabine ... because of the slow hydrolytic conversion of ancitabine to cytarabine. Check for active clinical trials using this agent. (NCI ... administration, ancitabine is slowly hydrolyzed into cytarabine. Subsequently, cytarabine is converted to the triphosphate form ...
Ancitabine (hydrochloride) Ipriflavone (S)-10-Hydroxycamptothecin Rotundine Guanosine Vanillin Empty. g. Empty. Astragaloside A ...
Ancitabine 31698-14-3 146. Andarine 401900-40-1 147. Andrographolide 5508-58-7 148. Androstenedione 63-05-8 149. ...
Ancitabine 31698-14-3 146. Andarine 401900-40-1 147. Andrographolide 5508-58-7 148. Androstenedione 63-05-8 149. ...
... pyrimidine analogs such as ancitabine, azacitidine, 6-azauridine, carmofur, cytarabine, dideoxyuridine, doxifluridine, ...
... pyrimidine analogs such as ancitabine, azacitidine, 6-azauridine, carmofur, cytarabine, dideoxyuridine, doxifluridine, ...
Upon administration, ancitabine is slowly hydrolyzed into cytarabi. T1600. Doxifluridine. Doxifluridine is a fluoropyrimidine ... Ancitabine Hydrochloride is the hydrochloride salt of a cytarabine congener prodrug with antineoplastic activity. ...
2) HILIC Ancitabine (hydrochloride)HPLC profiles of antithrombin specimens. rs762057and anti-FXa exercise (p = .02) (Desk two ...
Ancitabine hydrochloride C9H11N3O4.HCl 261.66. ...
Aqueous conversion kinetics and mechanisms of ancitabine, a prodrug of the antileukemic agent cytarabine. The addition of 8- ...
... pyrimidine analogs such as ancitabine, azacitidine, 6-azauridine, carmofur, cytarabine, dideoxyuridine, doxifluridine, ...
... analogs such as ancitabine, azacitidine, 6-azauridine, carmofur, cytarabine, dideoxyuridine, doxifluridine, enocitabine, ...
... pyrimidine analogs such as ancitabine, azacitidine, 6-azauridine, carmofur, cytarabine, dideoxyuridine, doxifluridine, ...
... pyrimidine analogs such as ancitabine, azacitidine, 6-azauridine, carmofur, cytarabine, dideoxyuridine, doxifluridine, ...
Acute Disease, Adult, Ancitabine, adverse effects, Antineoplastic Combined Chemotherapy Protocols, Cytarabine, Daunorubicin, ...
Ancitabine Synonyms:. Ancitabine hydrochloride; Cyclotidine; Cyclo-C; 2,2-Anhydro-(1-β-D-arabinofuranosyl) ...

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