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

Philip 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

doi:10.1016/j.bmcl.2007.02.075

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

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4378-81. doi: 10.1016/j.bmcl.2007.02.075. Epub 2007 Mar 3.

Affiliation

¹ Department of Chemistry Research, Bayer Research Center, 400 Morgan Lane, West Haven, CT 06516, USA. pcwickens@hotmail.com

PMID: 17574417
DOI: 10.1016/j.bmcl.2007.02.075

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.

MeSH terms

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

Substances

Antineoplastic Agents
Protein Kinase Inhibitors
Vascular Endothelial Growth Factor Receptor-2