Design,synthesis and biological activities of histone deacetylase inhibitors with new zinc binding group
作者单位：Department of Medicinal ChemistryChina Pharmaceutical University Department of PharmacologySchool of Pharmaceutical ScienceZhejiang University
会议名称：《2012长三角药物化学研讨会》
会议日期：2012年
学科分类：1007[医学-药学(可授医学、理学学位)] 100701[医学-药物化学] 10[医学]
摘 要：Histone deacetylases(HDACs) inhibition causes hyperacetylation of histones leading to apoptosis of tumor *** apoptotic effects have been linked to the modulation in the expression of several regulatory tumor suppressor genes caused by the modified status of histone acetylation,a key event in chromatin *** of previously reported HDACs inhibitors are hydroxamic acid derivatives, which could chelate the zinc ion in the active site in a bidentate ***,hydroxamic acids occasionally have produced problems such as poor pharmacokinetics,severe toxicity and low selectivity.