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

Producción científica: Article › revisión exhaustiva

45 Citas (Scopus)

Resumen

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.

Idioma original	English
Páginas (desde-hasta)	460-465
Número de páginas	6
Publicación	ACS Medicinal Chemistry Letters
Volumen	1
N.º	9
DOI	https://doi.org/10.1021/ml100083c
Estado	Published - dic 9 2010

ODS de las Naciones Unidas

Este resultado contribuye a los siguientes Objetivos de Desarrollo Sostenible

Good health and well being

ASJC Scopus subject areas

Biochemistry
Drug Discovery
Organic Chemistry

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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

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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\}",

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day = "9",

doi = "10.1021/ml100083c",

language = "English",

volume = "1",

pages = "460--465",

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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, n.º 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 - https://www.scopus.com/pages/publications/78650201913

UR - https://www.scopus.com/pages/publications/78650201913#tab=citedBy

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

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ASJC Scopus subject areas

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