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Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors

文献类型：期刊论文

作者Zhang, Shu-Wei2,4; Gong, Chao-Jun2; Su, Ming-Bo2; Chen, Fei2; He, Ting1; Zhang, Yang-Ming2,3; Shen, Qian-Qian1; Su, Yi1; Ding, Jian1; Li, Jia2
刊名JOURNAL OF MEDICINAL CHEMISTRY
出版日期2020-01-23
卷号63期号:2页码:804-815
ISSN号0022-2623
DOI10.1021/acs.jmedchem.9b01792
通讯作者Li, Jia(jli@simm.ac.cn) ; Chen, Yi(ychen@simm.ac.cn) ; Nan, Fa-Jun(fjnan@simm.ac.cn)
英文摘要A series of bisthiazole-based hydroxamic acids as novel potent HDAC inhibitors was developed during our previous work. In the present work, a new series of highly potent bisthiazole-based compounds were designed and synthesized. Among the prepared compounds, compound H13, which contains an alpha-(S)-methyl-substituted benzyl group, displays potent inhibitory activity toward human HDACs and several cancer cells lines. Compound H13 has a favorable PK profile and high tissue distribution specificity in the colon, as well as good efficacy in the AOM-DSS mouse model for colitis-associated colonic tumorigenesis.
WOS关键词T-CELL LYMPHOMA ; POTENT
资助项目National Natural Science Foundation of China[30725049] ; National Science and Technology Major Project[2018ZX09711002-011-006] ; Personalized Medicines Molecular Signature-Based Drug Discovery and Development, Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12020106] ; Shanghai Science and Technology Committee[19431906400]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000509438800020
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/282487]  
专题新药研究国家重点实验室
通讯作者Li, Jia; Chen, Yi; Nan, Fa-Jun
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, State Key Lab Drug Res, Shanghai 201203, Peoples R China
3.Yantai Inst Mat Med, Yantai Key Lab Nanomed & Adv Preparat, Yantai 264000, Shandong, Peoples R China
4.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714		 Zhang, Shu-Wei,Gong, Chao-Jun,Su, Ming-Bo,et al. Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors[J]. JOURNAL OF MEDICINAL CHEMISTRY,2020,63(2):804-815.
APA Zhang, Shu-Wei.,Gong, Chao-Jun.,Su, Ming-Bo.,Chen, Fei.,He, Ting.,...&Nan, Fa-Jun.(2020).Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors.JOURNAL OF MEDICINAL CHEMISTRY,63(2),804-815.
MLA Zhang, Shu-Wei,et al."Synthesis and in Vitro and in Vivo Biological Evaluation of Tissue-Specific Bisthiazole Histone Deacetylase (HDAC) Inhibitors".JOURNAL OF MEDICINAL CHEMISTRY 63.2(2020):804-815.

入库方式： OAI收割

来源：上海药物研究所

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