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Indolizine derivatives as HIV-1 VIF-ElonginC interaction inhibitors

Chem Biol Drug Des. 2013 Jun;81(6):730-41. doi: 10.1111/cbdd.12119.

Abstract

Compound 1 (VEC-5) was identified as a potent small-molecular HIV-1 viron infectivity factor inhibitor that targets the viron infectivity factor-ElonginC interaction. A structure-activity relationship study was carried out to develop compounds with improved efficacy against HIV-1 and 49 indolizine derivatives of three categories were designed and synthesized. We found that five compounds exhibited promising anti-HIV-1 activity, and the most active compound 2g had an IC50 value of 11.0 μm. These results provide new information to develop highly potent small-molecule HIV-1 viron infectivity factor inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemistry*
  • Anti-HIV Agents / metabolism
  • Anti-HIV Agents / pharmacology
  • Elongin
  • HIV-1 / drug effects
  • HIV-1 / metabolism*
  • Humans
  • Indolizines / chemistry*
  • Indolizines / metabolism
  • Indolizines / pharmacology
  • Protein Binding / drug effects
  • Structure-Activity Relationship
  • Transcription Factors / antagonists & inhibitors
  • Transcription Factors / metabolism*
  • vif Gene Products, Human Immunodeficiency Virus / antagonists & inhibitors
  • vif Gene Products, Human Immunodeficiency Virus / metabolism*

Substances

  • Anti-HIV Agents
  • Elongin
  • Indolizines
  • Transcription Factors
  • ethyl 3-(2-naphthoyl)-7-isonicotinoylindolizine-1-carboxylate
  • vif Gene Products, Human Immunodeficiency Virus
  • indolizine