Discovery of novel non-cytotoxic salicylhydrazide containing HIV-1 integrase inhibitors

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6472-5. doi: 10.1016/j.bmcl.2007.09.102. Epub 2007 Oct 10.

Abstract

The previously discovered salicylhydrazide class of compounds displayed potent HIV-1 integrase (IN) inhibitory activity. The development of this class of compounds as antiretroviral agents was halted due to cytotoxicity in the nanomolar to sub-micromolar range. We identified a novel class of non-cytotoxic hydrazide IN inhibitors utilizing the minimally required salicylhydrazide substructure as a template in a small-molecule database search. The novel hydrazides displayed low micromolar IN inhibitory activity and are several hundred-fold less cytotoxic than previously disclosed salicylhydrazide IN inhibitors.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • Cytotoxins / analysis
  • Cytotoxins / chemistry
  • Cytotoxins / pharmacology
  • Databases, Factual
  • HIV Integrase / metabolism*
  • HIV Integrase Inhibitors / analysis
  • HIV Integrase Inhibitors / chemistry*
  • HIV Integrase Inhibitors / pharmacology
  • Humans
  • Hydrazines / analysis
  • Hydrazines / chemistry*
  • Hydrazines / pharmacology

Substances

  • Cytotoxins
  • HIV Integrase Inhibitors
  • Hydrazines
  • salicyl hydrazide
  • HIV Integrase
  • p31 integrase protein, Human immunodeficiency virus 1