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Novel benzoyl thioureido benzene sulfonamides as high potent and selective inhibitors of carbonic anhydrase IX: structural optimization and bioactive studies

Abstract

CA IX has attracted much attention as a promising target for the development of new anticancer agents. In this study, a series of sulfonamides derivatives were designed and synthesized as potential CA IX inhibitors from a lead compound (benzoyl thioureido benzene sulfonamide) discovered by virtual screening. Bioassay demonstrated that some of the synthesized compounds exhibited potent inhibitory activity against CA IX in sub nanomolar range and high selectivity over the isozymes CA I and CA II. Among them, compound 6a displayed inhibitory activity against CA IX by IC50 0.48 nM and about 1500-fold selectivity over CA II. The structure-activity relationship and CA IX selectivity of the new sulfonamides derivatives were also analyzed by molecular docking results.

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Publication details

The article was received on 11 Aug 2018, accepted on 05 Nov 2018 and first published on 09 Nov 2018


Article type: Research Article
DOI: 10.1039/C8MD00392K
Citation: Med. Chem. Commun., 2018, Accepted Manuscript
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    Novel benzoyl thioureido benzene sulfonamides as high potent and selective inhibitors of carbonic anhydrase IX: structural optimization and bioactive studies

    Y. Xu, L. Liu, W. Wang, J. Huang, Z. Zhao and H. Li, Med. Chem. Commun., 2018, Accepted Manuscript , DOI: 10.1039/C8MD00392K

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