Inhibitors of anthrax lethal factor

  • Bioorg Med Chem Lett. 2007 Aug 15;17(16):4575-8. doi: 10.1016/j.bmcl.2007.05.089.
Brandon D Gaddis  1 ,  Larisa V Avramova ,  Jean Chmielewski
Affiliations
  • 1. Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
PMID: 17574849 DOI: 10.1016/j.bmcl.2007.05.089
Abstract

An inhibitor of anthrax lethal toxin mediated cell death (1) was identified by a medium throughput cell-based screen. This compound was determined to specifically inhibit anthrax lethal factor (LF), and subsequent SAR studies produced an even more potent inhibitor (4). Mechanistic studies identified these agents as uncompetitive inhibitors of LF with Ki values of 3.0 and 1.7 microM, respectively, with good cell potency and low cytotoxicity.