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SAR of a novel 'Anthranilamide Like' series of VEGFR-2, multi protein kinase inhibitors for the treatment of cancer.
Wickens, Philip; Kluender, Harold; Dixon, Julie; Brennan, Catherine; Achebe, Furahi; Bacchiocchi, Antonella; Bankston, Don; Bierer, Donald; Brands, Michael; Braun, Debbie; Brown, Melissa S; Chuang, Chih-Yuan; Dumas, Jacques; Enyedy, Istvan; Hofilena, Gloria; Hong, Zhenqiu; Housley, Tim; Jones, Benjamin; Khire, Uday; Kreiman, Charles; Kumarasinghe, Ellalahewage; Lowinger, Timothy; Ott-Morgan, Ronda; Perkins, Louise; Phillips, Barton; Schoenleber, Robert; Scott, William J; Sheeler, Ryan; Redman, Anikó; Sun, Xiuying; Taylor, Ian; Wang, Lei; Wilhelm, Scott; Zhang, Xiaomei; Zhang, Mingbao; Sullivan, Elizabeth; Carter, Christopher; Miglarese, Mark; Levy, Joan.
Bioorg Med Chem Lett ; 17(15): 4378-81, 2007 Aug 01.
Article in English | MEDLINE | ID: mdl-17574417

ABSTRACT

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.


Subject(s)
Antineoplastic Agents/pharmacology , Neoplasms/drug therapy , Protein Kinase Inhibitors/pharmacology , Vascular Endothelial Growth Factor Receptor-2/antagonists & inhibitors , Animals , Antineoplastic Agents/therapeutic use , Cell Line, Tumor , Humans , Mice , Protein Kinase Inhibitors/therapeutic use , Structure-Activity Relationship
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