2. Academic Validation
  3. Evaluation of Diarylureas for Activity Against Plasmodium falciparum

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

Affiliation

  • 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.

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