Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors |
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| Authors: | Ariamala Gopalsamy Greg Ciszewski Yongbo Hu Frederick Lee Larry Feldberg Eileen Frommer Steven Kim Karen Collins Donald Wojciechowicz Robert Mallon |
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| Institution: | 1. Chemical and Screening Sciences, Wyeth Research, 401 N. Middletown Road, Pearl River, NY 10965, USA;2. Discovery Oncology, Wyeth Research, 401 N. Middletown Road., Pearl River, NY 10965, USA |
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| Abstract: | B-Raf kinase plays a critical role in the Raf-MEK-ERK signaling pathway and inhibitors of B-Raf could be used in the treatment of melanomas, colorectal cancer, and other Ras related human cancers. We have identified novel small molecule pyrazolo1,5-a]pyrimidine derivatives as B-Raf kinase inhibitors. Structure–activity relationship was generated for various regions of the scaffold to improve the biochemical profile. |
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