Evaluation of Diarylureas for Activity Against Plasmodium falciparum

  • ACS Med Chem Lett. 2010 Dec 9;1(9):460-465. doi: 10.1021/ml100083c.
Yiqun Zhang  1 ,  Marc Anderson ,  Jennifer L Weisman ,  Min Lu ,  Cindy J Choy ,  Vincent A Boyd ,  Jeanine Price ,  Martina Sigal ,  Julie Clark ,  Michele Connelly ,  Fangyi Zhu ,  W Armand Guiguemde ,  Cynthia Jeffries ,  Lei Yang ,  Andrew Lemoff ,  Ally P Liou ,  Thomas R Webb ,  Joseph L Derisi ,  R Kiplin Guy
Affiliations
  • 1. Chemical Biology & Therapeutics Department, St Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105.
PMID: 21243104 DOI: 10.1021/ml100083c
Abstract

A library of diarylurea IGFR inhibitors was screened for activity against chloroquine-sensitive (3D7) and chloroquine-resistant (K1) strains of Plasmodium falciparum. The 4-aminoquinaldine-derived diarylureas displayed promising antimalarial potency. Further exploration of the B ring of 4-aminoquinaldinyl ureas allowed identification of several quinaldin-4-yl ureas 4{13, 39} and 4{13, 58} sufficiently potent against both 3D7 and K1 strains to qualify as bone fide leads.