Design and synthesis of a new generation of substituted purine hydroxamate analogs as histone deacetylase inhibitors

Bioorganic & Medicinal Chemistry
2016.0

Abstract

Histone deacetylase inhibitors have been proved to be great potential for the treatment of cancer. Recently, we designed and modified a series of substituted purine hydroxamate analogs as potent HDAC inhibitors based on our previous studies. The target compounds were investigated for their in vitro HDAC inhibitory activities and anti-proliferative activities. Results indicated that these compounds could effectively inhibit HDAC and possess obvious anti-proliferative activity against tumor cells. Promisingly, target compounds 4m and 4n outperformed SAHA in both enzymatic inhibitory activity and cellular anti-proliferative activity assay.

DOI： 10.1016/j.bmc.2016.02.005

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