Journal of heterocyclic chemistry

2??amino??4??oxo??6??substituted??pyrrolo [2, 3??d] pynmidines as potential inhibitors of thymidylate synthase

A Gangjee, J Yu, RL Kisliuk

文献索引：Gangjee, Aleem; Yu, Jianming; Kisliuk, Roy L. Journal of Heterocyclic Chemistry, 2002 , vol. 39, # 4 p. 833 - 840

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被引用次数: 21

摘要

Abstract Classical, antifolate inhibitors of thymidylate synthase often suffer from a number of potential disadvantages when used as antitumor agents. These include impaired uptake due to an alteration of the active transport system required for cellular uptake, as well as the formation of long acting, non-effluxing polygluta-mates via folypolyglutamate synthetase, which are responsible for toxicity to normal cells. To overcome some of the disadvantages ...