Identification of N-(6-mercaptohexyl)-3-(4-pyridyl)-1H-pyrazole-5-carboxamide and its disulfide prodrug as potent histone deacetylase inhibitors with in vitro and in vivo anti-tumor efficacy
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- 作者：Jiachen Wena ; 1 ; Yu Baob ; 1 ; Qun Niua ; Jinyu Yanga ; Yinbo Fana ; Jinhua Lia ; Yongkui Jingb ; c ; yongkui.jing@mssm.edu" class="auth_mail" title="E-mail the corresponding author ; Linxiang Zhaoa ; linxiang.zhao@vip.sina.com" class="auth_mail" title="E-mail the corresponding author ; Dan Liua ; sammyld@163.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：Histone deacetylase inhibitor ; Thiol ; Disulfide ; Prodrug ; Anti-tumor ; Structure-activity relationship
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：15 February 2016
- 年：2016
- 卷：109
- 期：Complete
- 页码：350-359
- 全文大小：1655 K
文摘
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A collection of novel thiol-based HDAC inhibitors was developed.
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Compound 15k and its analogs showed potent inhibition activity against HDAC1–3 and HDAC6.
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A sulfur-masked prodrug strategy was investigated for HDAC inhibitor.
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Disulfide 18 was identified as potent anti-tumor agent in vitro and in vivo.