Evaluation of diarylureas for activity against plasmodium falciparum

Yiqun Zhang, 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

Research output: Contribution to journalArticle

22 Citations (Scopus)

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.

Original languageEnglish (US)
Pages (from-to)460-465
Number of pages6
JournalACS Medicinal Chemistry Letters
Volume1
Issue number9
DOIs
StatePublished - Dec 9 2010

Fingerprint

Chloroquine
Plasmodium falciparum
Urea
Somatomedin Receptors
Antimalarials
Somatomedins
Libraries
Bone
Bone and Bones
4-amino-2-methylquinoline

Keywords

  • diarylurea
  • Malaria

ASJC Scopus subject areas

  • Organic Chemistry
  • Drug Discovery
  • Biochemistry

Cite this

Zhang, Y., Anderson, M., Weisman, J. L., Lu, M., Choy, C. J., Boyd, V. A., ... Guy, R. K. (2010). Evaluation of diarylureas for activity against plasmodium falciparum. ACS Medicinal Chemistry Letters, 1(9), 460-465. https://doi.org/10.1021/ml100083c

Evaluation of diarylureas for activity against plasmodium falciparum. / Zhang, Yiqun; Anderson, Marc; Weisman, Jennifer L.; Lu, Min; Choy, Cindy J.; Boyd, Vincent A.; Price, Jeanine; Sigal, Martina; Clark, Julie; Connelly, Michele; Zhu, Fangyi; Guiguemde, W. Armand; Jeffries, Cynthia; Yang, Lei; Lemoff, Andrew; Liou, Ally P.; Webb, Thomas R.; Derisi, Joseph L.; Guy, R. Kiplin.

In: ACS Medicinal Chemistry Letters, Vol. 1, No. 9, 09.12.2010, p. 460-465.

Research output: Contribution to journalArticle

Zhang, Y, Anderson, M, Weisman, JL, Lu, M, Choy, CJ, Boyd, VA, Price, J, Sigal, M, Clark, J, Connelly, M, Zhu, F, Guiguemde, WA, Jeffries, C, Yang, L, Lemoff, A, Liou, AP, Webb, TR, Derisi, JL & Guy, RK 2010, 'Evaluation of diarylureas for activity against plasmodium falciparum', ACS Medicinal Chemistry Letters, vol. 1, no. 9, pp. 460-465. https://doi.org/10.1021/ml100083c
Zhang Y, Anderson M, Weisman JL, Lu M, Choy CJ, Boyd VA et al. Evaluation of diarylureas for activity against plasmodium falciparum. ACS Medicinal Chemistry Letters. 2010 Dec 9;1(9):460-465. https://doi.org/10.1021/ml100083c
Zhang, Yiqun ; Anderson, Marc ; Weisman, Jennifer L. ; Lu, Min ; Choy, Cindy J. ; Boyd, Vincent A. ; Price, Jeanine ; Sigal, Martina ; Clark, Julie ; Connelly, Michele ; Zhu, Fangyi ; Guiguemde, W. Armand ; Jeffries, Cynthia ; Yang, Lei ; Lemoff, Andrew ; Liou, Ally P. ; Webb, Thomas R. ; Derisi, Joseph L. ; Guy, R. Kiplin. / Evaluation of diarylureas for activity against plasmodium falciparum. In: ACS Medicinal Chemistry Letters. 2010 ; Vol. 1, No. 9. pp. 460-465.
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