Design,Synthesis and Biological Evaluation of Novel Selective Thiol-based Histone Deacetylase(HDAC) VI InhibitorsBearing Indeno[1,2-c]pyrazole or Benzoindazole Scaffold |
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| Authors: | XU Qihao YU Shujia CAI Yijun YANG Jinyu ZHAO Linxiang LIU Dan |
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| Affiliation: | Key Laboratory of Structure-based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China |
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| Abstract: | A series of thiol-based indeno[1,2-c]pyrazoles and benzoindazole compounds was designed and synthesized according to the structural specificity of histone 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. |
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| Keywords: | Histone deacetylase VI(HDAC6) selective inhibitor Indeno[1 2-c]pyrazole compound Benzoindazole compound Antitumor |
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