SAR of a novel ‘Anthranilamide Like’ series of VEGFR-2, multi protein kinase inhibitors for the treatment of cancer

Novel series of anthranilamide type molecules that are active as inhibitors of B-RAF, c-KIT, and VEGFR-2 were identified. Novel anthranilamides were surprisingly found to exert additional activity on B-RAF. Corresponding thiophene, pyrazole, and thiazole core analogs were prepared as VEGFR-2 inhibit...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 17; no. 15; pp. 4378 - 4381
Main Authors:	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
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier Ltd 01-08-2007 Elsevier
Subjects:	Animals Anthranilamide Antineoplastic agents Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use Biological and medical sciences Cancer Cell Line, Tumor General aspects Humans Kinase Medical sciences Mice Neoplasms - drug therapy Pharmacology. Drug treatments Protein Kinase Inhibitors - pharmacology Protein Kinase Inhibitors - therapeutic use Structure-Activity Relationship Vascular Endothelial Growth Factor Receptor-2 - antagonists & inhibitors Kinase Anthranilamide Cancer Antineoplastic agent Angiogenic factor Thiazole derivatives Pyridine derivatives Vascularization Angiogenesis Thiophene derivatives Signal transduction Structure activity relation Pyrazole derivatives Ureas Neovascularization Antiangiogenic agent Chemical synthesis kit Gene Enzyme Transferases Rodentia Enzyme inhibitor Malignant tumor In vivo Vertebrata Growth factor receptor Mammalia Vascular endothelium growth factor Mouse Animal Inhibitor Fluorine Organic compounds
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Summary:	Novel series of anthranilamide type molecules that are active as inhibitors of B-RAF, c-KIT, and VEGFR-2 were identified. 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.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2007.02.075