Discovery of small-molecule inhibitors of the ATPase activity of human papillomavirus E1 helicase

被引：111

作者：

Faucher, AM ^{[1
]}

White, PW ^{[1
]}

Brochu, C ^{[1
]}

Grand-Maître, C ^{[1
]}

Rancourt, J ^{[1
]}

Fazal, G ^{[1
]}

机构：

[1] Boehringer Ingelheim Canada Ltd, Res & Dev, Laval, PQ H7S 2G5, Canada

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 47卷 / 01期

关键词：

D O I：

10.1021/jm034206x

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The Boehringer Ingelheim compound collection was screened for inhibitors of the ATPase activity of human papillomavirus El helicase to develop antiviral agents that inhibit human papillomavirus (HPV) DNA replication. This screen led to the discovery of (biphenyl-4-sulfonyl)acetic acid 1, which inhibits the ATPase activity of HPV type 6 E1 helicase with a low micromolar IC50 value. A hit-to-lead exercise rapidly converted 1 into a low nanomolar lead series.

引用

页码：18 / 21

页数：4

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