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

Publication ,  Journal Article
Smallheer, JM; Otto, MJ; Amaral-Ly, CA; Earl, RA; Myers, MJ; Pennev, P; Montefiori, DC; Wuonola, MA
Published in: Antiviral Chemistry and Chemotherapy
January 1, 1993

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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Published In

Antiviral Chemistry and Chemotherapy

DOI

ISSN

0956-3202

Publication Date

January 1, 1993

Volume

4

Issue

1

Start / End Page

27 / 39

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
 

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Smallheer, J. M., Otto, M. J., Amaral-Ly, C. A., Earl, R. A., Myers, M. J., Pennev, P., … Wuonola, M. A. (1993). Synthesis and anti-HIV activity of a series of 2-indolinones and related analogues. Antiviral Chemistry and Chemotherapy, 4(1), 27–39. https://doi.org/10.1177/095632029300400104
Smallheer, J. M., M. J. Otto, C. A. Amaral-Ly, R. A. Earl, M. J. Myers, P. Pennev, D. C. Montefiori, and M. A. Wuonola. “Synthesis and anti-HIV activity of a series of 2-indolinones and related analogues.” Antiviral Chemistry and Chemotherapy 4, no. 1 (January 1, 1993): 27–39. https://doi.org/10.1177/095632029300400104.
Smallheer JM, Otto MJ, Amaral-Ly CA, Earl RA, Myers MJ, Pennev P, et al. Synthesis and anti-HIV activity of a series of 2-indolinones and related analogues. Antiviral Chemistry and Chemotherapy. 1993 Jan 1;4(1):27–39.
Smallheer, J. M., et al. “Synthesis and anti-HIV activity of a series of 2-indolinones and related analogues.” Antiviral Chemistry and Chemotherapy, vol. 4, no. 1, Jan. 1993, pp. 27–39. Scopus, doi:10.1177/095632029300400104.
Smallheer JM, Otto MJ, Amaral-Ly CA, Earl RA, Myers MJ, Pennev P, Montefiori DC, Wuonola MA. Synthesis and anti-HIV activity of a series of 2-indolinones and related analogues. Antiviral Chemistry and Chemotherapy. 1993 Jan 1;4(1):27–39.
Journal cover image

Published In

Antiviral Chemistry and Chemotherapy

DOI

ISSN

0956-3202

Publication Date

January 1, 1993

Volume

4

Issue

1

Start / End Page

27 / 39

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