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

doi:10.1021/ml100083c

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

Biochemistry

Research output: Contribution to journal › Article › peer-review

41 Scopus citations

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 language	English (US)
Pages (from-to)	460-465
Number of pages	6
Journal	ACS Medicinal Chemistry Letters
Volume	1
Issue number	9
DOIs	https://doi.org/10.1021/ml100083c
State	Published - Dec 9 2010

Keywords

Malaria
diarylurea

ASJC Scopus subject areas

Biochemistry
Drug Discovery
Organic Chemistry

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10.1021/ml100083c

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Zhang, Y., Anderson, M., Weisman, J. L., Lu, M., Choy, C. J., Boyd, V. A., Price, J., Sigal, M., Clark, J., Connelly, M., Zhu, F., Guiguemde, W. A., Jeffries, C., Yang, L., Lemoff, A., Liou, A. P., Webb, T. R., Derisi, J. L., & 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

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

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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.",

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AU - Price, Jeanine

AU - Sigal, Martina

AU - Clark, Julie

AU - Connelly, Michele

AU - Zhu, Fangyi

AU - Guiguemde, W. Armand

AU - Jeffries, Cynthia

AU - Yang, Lei

AU - Lemoff, Andrew

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Evaluation of diarylureas for activity against plasmodium falciparum

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