A DIDEAZATETRAHYDROFOLATE ANALOG LACKING A CHIRAL CENTER AT C-6, N-[4-[2-(2-AMINO-3,4-DIHYDRO-4-OXO-7H-PYRROLO[2,3-D]PYRIMIDIN-5-YL)ETHYL]BENZOYL]-L-GLUTAMIC ACID, IS AN INHIBITOR OF THYMIDYLATE SYNTHASE

被引：277

作者：

TAYLOR, EC

KUHNT, D

SHIH, C

RINZEL, SM

GRINDEY, GB

BARREDO, J

JANNATIPOUR, M

MORAN, RG

机构：

[1] ELI LILLY & CO,LILLY RES LAB,LILLY CORP CTR,INDIANAPOLIS,IN 46285

[2] UNIV SO CALIF,DEPT BIOCHEM,LOS ANGELES,CA 90033

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 35卷 / 23期

关键词：

D O I：

10.1021/jm00101a023

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

N-[4-[2-(2-Amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid (15), prepared in five steps from 2-pivaloyl-7-deazaguanine, has been found to be an antitumor agent with its primary site of action at thymidylate synthase rather than purine synthesis. This compound appears to be a promising candidate for clinical evaluation.

引用

页码：4450 / 4454

页数：5

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