Evaluation of Diarylureas for Activity Against Plasmodium falciparum.
A library of diarylurea IGFR 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.
Chemical Biology & Therapeutics Department, St Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105.
Yiqun
Y
Zhang
Marc
M
Anderson
Jennifer L
JL
Weisman
Min
M
Lu
Cindy J
CJ
Choy
Vincent A
VA
Boyd
Jeanine
J
Price
Martina
M
Sigal
Julie
J
Clark
Michele
M
Connelly
Fangyi
F
Zhu
W Armand
WA
Guiguemde
Cynthia
C
Jeffries
Lei
L
Yang
Andrew
A
Lemoff
Ally P
AP
Liou
Thomas R
TR
Webb
Joseph L
JL
Derisi
R Kiplin
RK
Guy
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