Synthesis of 5-substituted quinazolinone derivatives and their inhibitory activity in vitro

被引：52

作者：

Baek, DJ ^{[1
]}

Park, YK ^{[1
]}

Heo, HI ^{[1
]}

Lee, MH ^{[1
]}

Yang, ZY ^{[1
]}

Choi, MH ^{[1
]}

机构：

[1] Choongwae Pharma Co, R&D Div, Res Lab, Drug Discovery Lab 1, Suwon, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 23期

关键词：

D O I：

10.1016/S0960-894X(98)00602-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Quinazolinone derivatives I and their methyl esters were synthesized and evaluated as nonclassical lipophilic inhibitors of thymidylate synthase. Compounds Ib and Ic containing OH and CO2H as R substituents, respectively, were most effective, indicating that hydrogen bonding may contribute to the increased inhibitory activity. These compounds further showed high cytotoxic activity against tumor cells in culture. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：3287 / 3290

页数：4

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