Synthesis of potent oxindole CDK2 inhibitors

被引：44

作者：

Dermatakis, A ^{[1
]}

Luk, KC ^{[1
]}

DePinto, W ^{[1
]}

机构：

[1] Hoffmann La Roche Inc, Nutley, NJ 07110 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2003年 / 11卷 / 08期

关键词：

D O I：

10.1016/S0968-0896(03)00036-1

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of oxindole CDK2 inhibitors was synthesized. These novel analogues have a saturated monosubstituted cyclic moiety at their C-4 position that mimics the ribofuranoside of ATP. This substitution afforded agents with increased potency relative to the parent indolinone and nanomolar range IC50 against the CDK2 enzyme and two cancer cell lines. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1873 / 1881

页数：9

共 18 条

[1] RAPID COLORIMETRIC ASSAY FOR CELL-GROWTH AND SURVIVAL - MODIFICATIONS TO THE TETRAZOLIUM DYE PROCEDURE GIVING IMPROVED SENSITIVITY AND RELIABILITY [J].