638-41-5Relevant articles and documents
Synthesis and biological activity evaluation of cytidine-5′-deoxy-5- fluoro-N-[(alkoxy/aryloxy)] carbonyl-cyclic 2′,3′-carbonates
Jhansi Rani,Raghavendra,Kishore,Nanda Kumar,Hema Kumar,Jagadeeswarareddy
experimental part, p. 690 - 696 (2012/09/08)
Capecitabine, an oral prodrug of 5-FU was developed to improve the tumor selectivity and tolerability. To enhance the efficacy of capacitabine, a series of 5′-deoxy-5-fluorocytidine derivatives 5a-e were synthesized. In the present study, we investigated antitumor activity of 5′-deoxy-5- fluorocytidine derivatives both in vivo and in vitro methods. Title compounds were non-mutagenic to Salmonella typhimurium tester strain in Ames test. Compounds 5d and 5e are potent to inhibit the proliferation of NCI-69, PZ-HPV-7, MCF-7 and HeLa cells in MTT assay. In particular, 5d and 5e showed potent antitumor activities against L1210 leukemia cell line. Collectively, these findings suggest that 5d and 5e are more potent anti-cancer compounds than capecitabine.
NOVEL VINBLASTINE DERIVATIVES, THEIR PREPARATION, USE AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAID DERIVATIVES
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Page/Page column 41, (2009/12/05)
The invention provides vinblastine derivatives represented by the following formula 1 or their physiologically acceptable salts, their preparation, use and pharmaceutical compositions comprising the said derivatives. The said vinblastine derivatives show inhibiting activities against tumor cell lines and can be used as medicaments for treating malignant tumors.
NOVEL DITHIOLOPYRROLONES AND THEIR THERAPEUTICAL APPLICATIONS
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Page/Page column 37, (2008/06/13)
The present invention provides novel dithiolopyrrolone compounds and their salts, which promote production of white blood cells and are useful as prevention and treatments for microbial infections such as HIV infection and blood disorders such as neutropenia and other related diseases. The present invention also provides therapeutic compositions comprising particularly useful types of dithiolopyrrolones, the salts thereof, and methods and use in the manufacture of a medication for treatment of diseases.
Preparation of chloroformates using bis(trichloromethyl)carbonate
Shi, Haibo,Hu, Weixiao,Sun, Yaquan
, p. 708 - 709 (2007/10/03)
The synthesis of eight chloroformates using bis(trichloromethyl) carbonate(BTC) is reported. It has been found that the yields by this BTC method are improved over the earlier phosgene method, and sodium hydroxide is better than pyridine as catalyst for the preparation of phenyl chloroformate.
KINETICS AND MECHANISM OF PHOSGENATION OF ALIPHATIC ALCOHOLS. IV. EFFECT OF HYDROGEN CHLORIDE ON THE REACTION RATE
Orlov, S. I.,Chimishkyan, A. L.,Stepanov, M. B.,Sidel'kovskii, A. L.,Grabarnik, M. S.,Elinevskii, A. V.
, p. 2278 - 2286 (2007/10/02)
The reaction of phosgene with alcohols is inhibited by hydrogen chloride.Here, as shown for the model methanolysis of methyl chloroformate, the halide ions have practically no effect on the reaction rate.The inhibition is due to the formation of associates, which do not possess nucleophilic characteristics between the alcohol and the hydrogen chloride.In proton-inert solvents at low temperatures the reaction only goes to the extent of a third on account of the formation of a stable unreactive 2:1 associate of the alcohol with hydrogen chloride.
1-Aziridine carboxylic acid derivatives with immunostimulant activity
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, (2008/06/13)
2-Substituted-1-aziridine-carboxylic acid esters exhibiting immuno-stimulant activity and of the formula STR1 wherein X is a carbamoyl or alkoxycarbonyl radical, and R1 is an aliphatic hydrocarbon radical optionally substituted by halogen, alkoxy, amino, carbamoyloxy, cycloalkyl, hydroxyl, an imido or heterocyclic radical, cycloalkyl; or aryl, aralkyl, aryloxyalkyl or arylthioalkyl wherein the aryl moiety is optionally substituted by halogen, alkyl, alkoxy, hydroxyl, amino, nitro, cyano, acyl, carbalkoxy, thioalkyl, alkylsulphonyl, phenyl or trifluoromethyl. Counterparts where X is --CN and R1 is as above, except for ethyl, are also new.
