Discovery and structural optimization of pyrazole derivatives as novel inhibitors of Cdc25B

HJ Chen, Y Liu, LN Wang, Q Shen, J Li…

Index: Chen, Hai-Jun; Liu, Yong; Wang, Li-Na; Shen, Qiang; Li, Jia; Nan, Fa-Jun Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 9 p. 2876 - 2879

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Citation Number: 10

Abstract

Structural optimization and preliminary structure–activity relationship studies of a series of N- substituted maleimide fused-pyrazole analogues with Cdc25B inhibitory activity, starting from a high-throughput screening hit, are illustrated. A simplified 3, 5-diacyl pyrazole analogue was obtained as the most potent compound (118, IC50= 0.12 μM) with a 270-fold increase in potency.