Synthesis of apicidin-derived quinolone derivatives: Parasite-selective histone deacetylase inhibitors and antiproliferative agents

被引：53

作者：

Meinke, PT ^{[1
]}

Colletti, SL ^{[1
]}

Doss, G ^{[1
]}

Myers, RW ^{[1
]}

Gurnett, AM ^{[1
]}

Dulski, PM ^{[1
]}

Darkin-Rattray, SJ ^{[1
]}

Allocco, JJ ^{[1
]}

Galuska, S ^{[1
]}

Schmatz, DM ^{[1
]}

Wyvratt, MJ ^{[1
]}

Fisher, MH ^{[1
]}

机构：

[1] Merck Res Labs, Rahway, NJ 07065 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2000年 / 43卷 / 25期

关键词：

D O I：

10.1021/jm0001976

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Apicidin's indole was efficiently converted into a series of N-substituted quinolone derivatives by indole N-alkylation followed by a two-step, one-pot, ozonolysis/aldol condensation protocol. The new quinolones exhibited good parasite selectivity and potency both at the level of their molecular target, histone deacetylase, and in their whole cell antiproliferative activity in vitro.

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页码：4919 / 4922

页数：4

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