Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors

被引：142

作者：

Skalitzky, DJ

Marakovits, JT

Maegley, KA

Ekker, A

Yu, XH

Hostomsky, Z

Webber, SE

Eastman, BW

Almassy, R

Li, JK

Curtin, NJ

Newell, DR

Calvert, AH

Griffin, RJ

Golding, BT

机构：

[1] Pfizer Global R&D, La Jolla Agouron Pharmaceut Inc, San Diego, CA 92121 USA

[2] Pharmaceut Inc, San Diego, CA 92121 USA

[3] Univ Newcastle Upon Tyne, Canc Res Unit, Newcastle Upon Tyne NE2 4HH, Tyne & Wear, England

[4] Univ Newcastle Upon Tyne, Dept Chem, Newcastle Upon Tyne NE1 7RU, Tyne & Wear, England

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 02期

关键词：

D O I：

10.1021/jm0255769

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel tricyclic benzimidazole carboxamide poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors have been synthesized. Several compounds were found to be powerful chemopotentiators of temozolomide and topotecan in both A549 and LoVo cell lines. In vitro inhibition of PARP-1 was confirmed by direct measurement of NAD(+) depletion and ADPribose polymer formation caused by chemically induced DNA damage.

引用

页码：210 / 213

页数：4

共 19 条

[1] LABELING METHODS FOR THE STUDY OF POLY(ADP-RIBOSE) AND MONO(ADP-RIBOSE) METABOLISM IN CULTURED-CELLS [J].