化学
药效团
心脏毒性
HDAC6型
双功能
癌症
生物化学
药理学
有机化学
组蛋白脱乙酰基酶
内科学
毒性
医学
基因
组蛋白
催化作用
作者
Feifei Yang,Бо Лю,Xue-Li Xu,Ting Hu,Jian‐Quan Liu,Zhangxu He,Guangyuan Zhao,Bo Wei,Liying Ma
标识
DOI:10.1021/acs.jmedchem.4c01168
摘要
Cardiotoxicity associated with chemotherapy has gradually become the major cause of death in cancer patients. The development of bifunctional drugs with both cardioprotective and antitumor effects has become the future direction. HDAC6 plays important roles in the progression, treatment, and prognosis of cancer and cardiovascular diseases, but bifunctional inhibitors have not been reported. Herein, structure-activity relationship studies driven by pharmacophore-based remodification and fragment-based design were performed to yield highly potent HDAC6 inhibitor
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