Synthesis of selenophene derivatives as novel CHK1 inhibitors

PC Hong, LJ Chen, TY Lai, HY Yang, SJ Chiang…

Index: Hong, Pao-Chiung; Chen, Li-Jung; Lai, Tzu-Yun; Yang, Huei-Yu; Chiang, Shih-Jan; Lu, Yann-Yu; Tsai, Ping-Kuei; Hsu, Hung-Yi; Wei, Win-Yin; Liao, Chu-Bin Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 17 p. 5065 - 5068

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Citation Number: 11

Abstract

A series of selenophene derivatives 3 were synthesized as potential CHK1 inhibitors. The effects of substitution on the 4′-or 5′-position of selenophene moiety and shifting the hydroxyl group position on C6-phenolic ring of oxindole were explored. This study led to the discovery of the most potent CHK1 inhibitors 29–33 and 39–43, which had IC50 values in the subnanomolar range.