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American Chemical Society, ACS Medicinal Chemistry Letters, 9(1), p. 460-465, 2010

DOI: 10.1021/ml100083c

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Evaluation of Diarylureas for Activity Against Plasmodium falciparum

Journal article published in 2010 by Yiqun Zhang, Marc Anderson, Jennifer L. Weisman, Min Lu, Cindy J. Choy, Vincent A. Boyd, Jeanine Price, Martina Sigal, Julie Clark, Michele Connelly, W. Armand Guiguemde, Fangyi Zhu, W. Armand Guiguemde, Cynthia Jeffries, Lei Yang and other authors.
This paper is available in a repository.
This paper is available in a repository.

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Abstract

A library of diarylurea insulin-like growth factor 1 receptor 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.