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

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

42 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
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

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.1021/ml100083c

Cite this

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

@article{62ced8c86a9546d6889034ee8c52e0fe,

title = "Evaluation of diarylureas for activity against plasmodium falciparum",

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.",

keywords = "Malaria, diarylurea",

author = "Yiqun Zhang and Marc Anderson and Weisman, {Jennifer L.} and Min Lu and Choy, {Cindy J.} and Boyd, {Vincent A.} and Jeanine Price and Martina Sigal and Julie Clark and Michele Connelly and Fangyi Zhu and Guiguemde, {W. Armand} and Cynthia Jeffries and Lei Yang and Andrew Lemoff and Liou, {Ally P.} and Webb, {Thomas R.} and Derisi, {Joseph L.} and Guy, {R. Kiplin}",

year = "2010",

month = dec,

day = "9",

doi = "10.1021/ml100083c",

language = "English",

volume = "1",

pages = "460--465",

number = "9",

}

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

TY - JOUR

T1 - Evaluation of diarylureas for activity against plasmodium falciparum

AU - Zhang, Yiqun

AU - Anderson, Marc

AU - Weisman, Jennifer L.

AU - Lu, Min

AU - Choy, Cindy J.

AU - Boyd, Vincent A.

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

AU - Liou, Ally P.

AU - Webb, Thomas R.

AU - Derisi, Joseph L.

AU - Guy, R. Kiplin

PY - 2010/12/9

Y1 - 2010/12/9

N2 - 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.

AB - 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.

KW - Malaria

KW - diarylurea

UR - http://www.scopus.com/inward/record.url?scp=78650201913&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=78650201913&partnerID=8YFLogxK

U2 - 10.1021/ml100083c

DO - 10.1021/ml100083c

M3 - Article

AN - SCOPUS:78650201913

VL - 1

SP - 460

EP - 465

JO - ACS Medicinal Chemistry Letters

JF - ACS Medicinal Chemistry Letters

IS - 9

ER -

Evaluation of diarylureas for activity against plasmodium falciparum

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

Access to Document

Other files and links

Fingerprint

Cite this