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 ...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.展开更多
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 ）.
文摘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.
