Cyclopenta[g]quinazoline-based antifolates:: The effect of the chirality at the 6-position on the inhibition of thymidylate synthase (TS)

被引：7

作者：

Bavetsias, V ^{[1
]}

Marriott, JH ^{[1
]}

Theti, DS ^{[1
]}

Melin, JC ^{[1
]}

Wilson, SC ^{[1
]}

Jackman, AL ^{[1
]}

机构：

[1] Inst Canc Res, Dept Chem, CRC Lab, CRC,Ctr Canc Therapeut, Sutton SM2 5NG, Surrey, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 23期

关键词：

D O I：

10.1016/S0960-894X(01)00612-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Cyclopenta[g]quinazoline-based inhibitors of thymidylate synthase (TS) possess a chiral centre at the 6-position of the molecule. The effect of this chirality on the inhibition of TS was investigated by synthesising compounds 6S-1a-c, 6R-1a-C. It was shown, in particular with the diastereoisomers 6S-1c, 6R-1c, that the inhibitory activity against TS is mainly due to the 6S diastereoisomer rather than the 6R diastereoisomer, which is virtually inactive. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：3015 / 3017

页数：3

共 8 条

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