Pyrrolo [2, 3-d] pyrimidine thymidylate synthase inhibitors: design and synthesis of one-carbon bridge derivatives.

…, Y Imai, K Yukishige, K Ootsu, H Akimoto

文献索引：Aso; Imai; Yukishige; Ootsu; Akimoto Chemical and Pharmaceutical Bulletin, 2001 , vol. 49, # 10 p. 1280 - 1287

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被引用次数: 15

摘要

A series of novel pyrrolo [2, 3-d] pyrimidine derivatives was designed and synthesized as thymidylate synthase (TS) inhibitors. Molecular design was performed on the human TS complex model built on the basis of the reported structure of TS- deoxyuridinemonophosphate (dUMP)-CB3717 ternary complex. From a docking study, we expected that a one-carbon bridge between pyrrolo [2, 3-d] pyrimidine and an aromatic ...