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…

Index: 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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Citation Number: 5

Abstract

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 ...