Synthesis and anti-HIV activity of a series of 2-indolinones and related analogues

Journal Article (Journal Article)

A novel series of 2-indolinones with in vitro anti-HIV (human immunodeficiency virus) activity is described. Two structurally related compound, 1, 3,3-(4-N-methyl-1,2,5,6-tetrahydropyridylmethyl)-1-phenyl-2- indolinone, and 2, its 4-N-methylpiperidinylmethyl analogue, 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 HV(IIIb) in cell protection assays with IC90 values of 4.4 and 14.9 μM (2.2 and 7.9 μg 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.

Full Text

Duke Authors

Cited Authors

  • Smallheer, JM; Otto, MJ; Amaral-Ly, CA; Earl, RA; Myers, MJ; Pennev, P; Montefiori, DC; Wuonola, MA

Published Date

  • January 1, 1993

Published In

Volume / Issue

  • 4 / 1

Start / End Page

  • 27 - 39

International Standard Serial Number (ISSN)

  • 0956-3202

Digital Object Identifier (DOI)

  • 10.1177/095632029300400104

Citation Source

  • Scopus