Bioorganic and Medicinal Chemistry p. 4364 - 4374 (2015)
Update date:2022-07-29
Topics:
Wang, Lei
Hou, Xuben
Fu, Huansheng
Pan, Xiaole
Xu, Wenfang
Tang, Weiping
Fang, Hao
Inhibition of HDACs activity has become a promising therapeutic strategy in clinical practice to reverse the abnormal epigenetic states of cancer and other diseases. Therefore, HDAC inhibitors become a relatively new class of anti-cancer agent. In the present study, we reported the design and synthesis of a series of novel HDAC inhibitors using various substituted quinoline rings as the cap group. In vitro studies showed that some compounds have good inhibitory activities against HDACs and potent antiproliferative activities in some tumor cell lines. Especially, compound 9w (IC50 = 85 nM), exhibited better inhibitory effect compared with SAHA (IC50 = 161 nM).
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