SYNTHESIS AND ANTI-HIV ACTIVITY OF A SERIES OF 2-INDOLINONES AND RELATED ANALOGS

被引：17

作者：

SMALLHEER, JM ^{[1
]}

OTTO, MJ ^{[1
]}

AMARALLY, CA ^{[1
]}

EARL, RA ^{[1
]}

MYERS, MJ ^{[1
]}

PENNEV, P ^{[1
]}

MONTEFIORI, DC ^{[1
]}

WUONOLA, MA ^{[1
]}

机构：

[1] VANDERBILT UNIV,MED CTR,SCH MED,DEPT PATHOL,NASHVILLE,TN 37232

来源：

ANTIVIRAL CHEMISTRY & CHEMOTHERAPY | 1993年 / 4卷 / 01期

关键词：

D O I：

10.1177/095632029300400104

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 novel series of 2-indolinones with in vitro anti-HIV (human immunodeficiency virus) activity is described. Two structurally related compounds, 1, 3,3-(4-N-methyl-1,2,5,6-tetrahydropyridylmethyl)-1- phenyl-2-indolinone, and 2, its 4-N-methylpiperidinylmethyl analogue (Fig. 1), formed the basis of a structure-activity study. The synthesis of approximately 50 analogues and their respective activities vs. HIV are presented. Both 1 and 2 were effective inhibitors of HIV(IIIb) in cell protection assays with IC90 values of 4.4 and 14.9 muM (2.2 and 7.9 mug ml-1), respectively. In the same concentration range, 1 and 2 also inhibit syncytia formation. These compounds represent a novel class of anti-HIV agents which appear to act by inhibiting virus-dependent cell fusion.

引用

页码：27 / 39

页数：13

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