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

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.
AuthorsPhilip Wickens, Harold Kluender, Julie Dixon, Catherine Brennan, Furahi Achebe, Antonella Bacchiocchi, Don Bankston, Donald Bierer, Michael Brands, Debbie Braun, Melissa S Brown, Chih-Yuan Chuang, Jacques Dumas, Istvan Enyedy, Gloria Hofilena, Zhenqiu Hong, Tim Housley, Benjamin Jones, Uday Khire, Charles Kreiman, Ellalahewage Kumarasinghe, Timothy Lowinger, Ronda Ott-Morgan, Louise Perkins, Barton Phillips, Robert Schoenleber, William J Scott, Ryan Sheeler, Anikó Redman, Xiuying Sun, Ian Taylor, Lei Wang, Scott Wilhelm, Xiaomei Zhang, Mingbao Zhang, Elizabeth Sullivan, Christopher Carter, Mark Miglarese, Joan Levy
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 17 Issue 15 Pg. 4378-81 (Aug 01 2007) ISSN: 0960-894X [Print] England
PMID17574417 (Publication Type: Journal Article)
Chemical References
  • Antineoplastic Agents
  • Protein Kinase Inhibitors
  • Vascular Endothelial Growth Factor Receptor-2
Topics
  • Animals
  • Antineoplastic Agents (pharmacology, therapeutic use)
  • Cell Line, Tumor
  • Humans
  • Mice
  • Neoplasms (drug therapy)
  • Protein Kinase Inhibitors (pharmacology, therapeutic use)
  • Structure-Activity Relationship
  • Vascular Endothelial Growth Factor Receptor-2 (antagonists & inhibitors)

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