A novel inhibitor of human telomerase derived from 10H-indolo[3,2-b]quinoline

被引：104

作者：

Caprio, V

Guyen, B

Opoku-Boahen, Y

Mann, J

Gowan, SM

Kelland, LM

Read, MA

Neidle, S

机构：

[1] Inst Canc Res, Chester Beatty Labs, CRC, Biomol Struct Unit, London SW3 6JB, England

[2] Inst Canc Res, CRC, Ctr Canc Therapeut, Sutton SM2 5NG, Surrey, England

[3] Queens Univ Belfast, Sch Chem, Belfast BT9 5AG, Antrim, North Ireland

[4] Univ Reading, Dept Chem, Reading RG6 6AD, Berks, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 18期

关键词：

D O I：

10.1016/S0960-894X(00)00378-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The bis-dimethylaminoethyl derivative of quindoline (10H-indolo[3,2-b]quinoline), an alkaloid from the West African shrub Cryptolepis sanguinolenta, has been synthesised. This has been shown to have modest cytotoxicity, as well as inhibitory activity against the telomerase enzyme. It is hypothesised that the latter activity is due to stabilisation of an intermediate guanine-quadruplex complex, in accordance with computer modelling. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2063 / 2066

页数：4

共 39 条

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