Discovery of the First N-Hydroxycinnamamide-Based Hydroxamic Acids with Dual HDAC1/3 Selectivity

来源 :全国药物化学学术会议暨第四届中英药物化学学术会议 | 被引量 : 0次 | 上传用户：jdwenge

【摘要】

：

【作者】

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Xiaoyang Li C.James Chou Xiaoguang Li Yingjie Zhang Wenfang Xu

【机构】

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Department of Medicinal Chemistry,School of Pharmaceutical Sciences,Shandong University,44 West Cult

【出处】

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全国药物化学学术会议暨第四届中英药物化学学术会议

【发表日期】

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2013年11期

【关键词】

：

HDACs inhibitor selectivity HDAC1 HDAC3

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　　In the past 10 years,over 490 clinical trials of more than 20 HDACs inhibitors(HDACIs)candidates have been initiated,culminating in the approval of three anti-tumor drugs vorinostat(SAHA),romidepsin(FK228)and Resminostat(4SC-201).In our previous study,we designed and synthesized a novel series of N-hydroxycinnamamide-based HDACIs combining indole bioactive fragment1.Further derivatization of these compounds led to a series of more potent N-hydroxycinnamamide-based HDACIs with promising in vivo antitumour activity.

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Discovery of the First N-Hydroxycinnamamide-Based Hydroxamic Acids with Dual HDAC1/3 Selectivity

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