Optimization of heterocyclic substituted benzenesulfonamides as novel carbonic anhydrase IX inhibitors and their structure activity relationship

…, W Zhu, L Wang, J Huang, Z Zhao, H Li, X Qian…

文献索引：Gao, Rui; Liao, Sha; Zhang, Chen; Zhu, Weilong; Wang, Liyan; Huang, Jin; Zhao, Zhenjiang; Li, Honglin; Qian, Xuhong; Xu, Yufang European Journal of Medicinal Chemistry, 2013 , vol. 62, p. 597 - 604

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被引用次数: 5

摘要

In this study, starting from a lead compound discovered by virtual screening, a series of novel heterocyclic substituted benzenesulfonamides were designed and synthesized as new carbonic anhydrase IX (CA IX) inhibitors. Some compounds exhibited potent inhibitory effects against CA IX (in the low nanomolar range) as well as high selectivity against other carbonic anhydrase isozymes (CA I and CA II). The most potent and selective compound ...