Inhibition of human immunodeficiency virus type (HIV-1) replication by some diversely functionalized spirocyclopropyl derivatives

Arch Pharm (Weinheim). 1999 May;332(5):163-6. doi: 10.1002/(sici)1521-4184(19995)332:5<163::aid-ardp163>3.0.co;2-2.

Abstract

Inhibition of HIV-1 replication by differently substituted spirocyclopropyl compounds has been evaluated. Compound 21 showed a moderate activity (EC50 ranging from 2.3 to 5.8 micrograms/ml) against different HIV-1 strains (IIIB, RF, NDK, and an AZT-resistant strain) in different cell lines (MT-4 and C-8166 cells), while it was cytotoxic at 77.7 micrograms/ml, resulting in a selectivity index of 34. This compound was inactive against HIV-2 (ROD) and SIV (MAC251). From "time-of-addition" experiments compound 21, like AZT, appeared to inhibit HIV-1 at the reverse transcriptase step.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology*
  • Cell Line
  • Cyclopropanes / chemical synthesis
  • Cyclopropanes / chemistry
  • Cyclopropanes / pharmacology*
  • HIV-1 / drug effects*
  • HIV-1 / physiology
  • HIV-2 / drug effects
  • Humans
  • Simian Immunodeficiency Virus / drug effects
  • Spiro Compounds / chemical synthesis
  • Spiro Compounds / chemistry
  • Spiro Compounds / pharmacology*
  • Structure-Activity Relationship
  • Virus Replication / drug effects*

Substances

  • Anti-HIV Agents
  • Cyclopropanes
  • Spiro Compounds