Synthesis and anti-HIV activity of a series of 2-indolinones and related analogues
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.
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- Virology
- 3404 Medicinal and biomolecular chemistry
- 1117 Public Health and Health Services
- 0601 Biochemistry and Cell Biology
- 0304 Medicinal and Biomolecular Chemistry
Citation
Published In
DOI
ISSN
Publication Date
Volume
Issue
Start / End Page
Related Subject Headings
- Virology
- 3404 Medicinal and biomolecular chemistry
- 1117 Public Health and Health Services
- 0601 Biochemistry and Cell Biology
- 0304 Medicinal and Biomolecular Chemistry