SAR of a novel 'Anthranilamide Like' series of VEGFR-2, multi protein kinase inhibitors for the treatment of cancer.
Novel anthranilamides were surprisingly found to exert additional activity on B-RAF. Corresponding thiophene, pyrazole, and thiazole core analogs were prepared as VEGFR-2 inhibitors with c-KIT, and B-RAF activity. Compounds in the phenyl, thiophene, and thiazole series are in vivo active.
Wickens
Philip
P
Department of Chemistry Research, Bayer Research Center, 400 Morgan Lane, West Haven, CT 06516, USA. pcwickens@hotmail.com
Kluender
Harold
H
Dixon
Julie
J
Brennan
Catherine
C
Achebe
Furahi
F
Bacchiocchi
Antonella
A
Bankston
Don
D
Bierer
Donald
D
Brands
Michael
M
Braun
Debbie
D
Brown
Melissa S
MS
Chuang
Chih-Yuan
CY
Dumas
Jacques
J
Enyedy
Istvan
I
Hofilena
Gloria
G
Hong
Zhenqiu
Z
Housley
Tim
T
Jones
Benjamin
B
Khire
Uday
U
Kreiman
Charles
C
Kumarasinghe
Ellalahewage
E
Lowinger
Timothy
T
Ott-Morgan
Ronda
R
Perkins
Louise
L
Phillips
Barton
B
Schoenleber
Robert
R
Scott
William J
WJ
Sheeler
Ryan
R
Redman
Anikó
A
Sun
Xiuying
X
Taylor
Ian
I
Wang
Lei
L
Wilhelm
Scott
S
Zhang
Xiaomei
X
Zhang
Mingbao
M
Sullivan
Elizabeth
E
Carter
Christopher
C
Miglarese
Mark
M
Levy
Joan
J
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D045744:Cell Line, Tumor; D006801:Humans; D051379:Mice; D009369:Neoplasms / Q000188:drug therapy*; D047428:Protein Kinase Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors*
D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D040301:Vascular Endothelial Growth Factor Receptor-2