AUTHOR=He Junquan , Wang Songsong , Liu Xingang , Lin Ruili , Deng Fang , Jia Zhong , Zhang Chenghong , Li Zhao , Zhu Hongtian , Tang Lei , Yang Pingrong , He Dian , Jia Qingzhong , Zhang Yang TITLE=Synthesis and Biological Evaluation of HDAC Inhibitors With a Novel Zinc Binding Group JOURNAL=Frontiers in Chemistry VOLUME=8 YEAR=2020 URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2020.00256 DOI=10.3389/fchem.2020.00256 ISSN=2296-2646 ABSTRACT=
Vorinostat (SAHA) with great therapeutic potential has been approved by the FDA for the treatment of cutaneous T-cell lymphoma as the first HDACs inhibitor, but the drawbacks associated with hydroxamic acid group (poor stability, easy metabolism, weak binding ability to class IIa isozymes, and poor selectivity) have been exposed during the continuous clinical application. Based on the pharmacophore of HDAC inhibitors, two series of compounds with novel zinc binding group (ZBG) were designed and synthesized, and the antitumor bioactivities were evaluated in four human cancer cell lines (A549, Hela, HepG2, and MCF-7). Among the synthesized compounds, compounds