Design, synthesis and biological evaluation of novel selective thiol-based histone deacetylase(HDAC) VI inhibitors bearing indeno[1,2-c]pyrazole or benzoindazole scaffold

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...

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Bibliographic Details
Published in:Chemical research in Chinese universities 2018-02, Vol.34 (1), p.75-83
Main Authors: Xu, Qihao, Yu, Shujia, Cai, Yijun, Yang, Jinyu, Zhao, Linxiang, Liu, Dan
Format: Article
Language:English
Subjects:
Analytical Chemistry
Chemistry
Chemistry and Materials Science
Chemistry/Food Science
Chromatin
Compound A
Fluorescence
Inhibitors
Inorganic Chemistry
Organic Chemistry
Physical Chemistry
Pyrazole
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Summary: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(IC 50 =44—598 nmol/L). Among them, compound A-4 displayed the highest selectivity against HDAC6 and similar inhibitory activity(IC 50 =44 nmol/L) to that of the positive drug SAHA(IC 50 =41 nmol/L) against HDAC6.
ISSN:1005-9040
2210-3171
DOI:10.1007/s40242-018-7239-6