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Design, Synthesis and Biological Evaluation of Novel Selective Thiol-based Histone Deacetylase(HDAC) Ⅵ Inhibitors Bearing Indeno[1,2-c]pyrazole or Benzoindazole Scaffold

Design, Synthesis and Biological Evaluation of Novel Selective Thiol-based Histone Deacetylase(HDAC) Ⅵ Inhibitors Bearing Indeno[1,2-c]pyrazole or Benzoindazole Scaffold
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摘要 A series of thiol-based mdeno[1,2-c]pyrazoles and benzoindazole compounds was designed and synthesized according to the structural specificity of his-tone deacetylase VI(HDAC6) and the structural characteristics of HDAC inhibitors. The inhibitory activities of the target compounds against HDAC6 and HDAC1 were screened by fluorescence analysis. Most of the target compounds showed moderate inhibitory activity against HDAC6(IC50=44-598 nmol/L). Among them, compound A-4 displayed the highest selectivity against HDAC6 and similar inhibitory activity(IC50=44 nmol/L) to that of the positive drug SAHA(IC50=41 nmol/L) against HDAC6. A series of thiol-based mdeno[1,2-c]pyrazoles and benzoindazole compounds was designed and synthesized according to the structural specificity of his-tone deacetylase VI(HDAC6) and the structural characteristics of HDAC inhibitors. The inhibitory activities of the target compounds against HDAC6 and HDAC1 were screened by fluorescence analysis. Most of the target compounds showed moderate inhibitory activity against HDAC6(IC50=44-598 nmol/L). Among them, compound A-4 displayed the highest selectivity against HDAC6 and similar inhibitory activity(IC50=44 nmol/L) to that of the positive drug SAHA(IC50=41 nmol/L) against HDAC6.
出处 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2018年第1期75-83,共9页 高等学校化学研究(英文版)
基金 Supported by the National Natural Science Foundation of China(No.81473086) and the Natural Science Foundation of Liaoning Province, China(No.2015020728 -301 ).
关键词 Histone deacetylase Ⅵ(HDAC6) selective inhibitor Indeno[1 2-c]pyrazole compound Benzoindazole compound ANTITUMOR Histone deacetylase Ⅵ(HDAC6) selective inhibitor, Indeno[1,2-c]pyrazole compound Benzoindazole compound Antitumor
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