B-Raf kinase inhibitors: Hit enrichment through scaffold hopping

Ariamala Gopalsamy,Mengxiao Shi,Yongbo Hu,Frederick Lee,Larry Feldberg,Eileen Frommer,Steven Kim,Karen Collins,Donald Wojciechowicz,Robert Mallon

Bioorganic & Medicinal Chemistry Letters（2010）

Cited 21|Views38

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Abstract

Scaffold hopping strategy was employed to replace the HTS hit scaffold pyrazolo[1,5-a]pyrimidine. This strategy led to the identification of additional lead compound 11b with enhanced enzyme and cellular potency, while maintaining good selectivity over a number of kinases.

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Key words

B-Raf kinase,Thienopyrimidine

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