Bioorganic and Medicinal Chemistry Letters p. 2136 - 2140 (2019)
Update date:2022-09-26
Topics:
Yu, Yu
Ran, Dongzhi
Jiang, Junhao
Pan, Tao
Dan, Yanrong
Tang
Li, Wei
Zhang, Lin
Gan, LinLing
Gan, Zongjie
HDAC and CDK inhibitors have been demonstrated to be synergistically in suppressing cancer cell proliferation and inducing apoptosis. In this work, we incorporated the pharmacophore groups of HDACs and CDKs inhibitors into one molecule to design and synthesize a series of purin derivatives as HDAC/CDK dual inhibitors. The lead compound 6d, showing good HDAC1 and CDK2 inhibitory activity with IC50 values of 5.8 and 56 nM, respectively, exhibited attractive potency against several cancer cell lines in vitro. This work may lead to the discovery of a novel scaffold and potential dual HDAC/CDK inhibitors.
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