Novel indolin-2-one-based sulfonamides as carbonic anhydrase inhibitors: Synthesis, in vitro biological evaluation against carbonic anhydrases isoforms I, II, IV and VII and molecular docking studies

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• 作者：Wagdy M. Eldehna^a ; ^{wagdy2000@gmail.com} ; Ghada H. Al-Ansary^b ; Silvia Bua^c ; Alessio Nocentini^c ; ^d ; Paola Gratteri^d ; Ayman Altoukhy^e ; Hazem Ghabbour^f ; ^g ; Hanaa Y. Ahmed^h ; Claudiu T. Supuran^c ; ^{claudiu.supuran@unifi.it}
• 关键词：Synthesis ; Carbonic anhydrase ; 4-(2-Aminoethyl)benzenesulfonamide ; Isatin
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：521-530
• 全文大小：1362 K
• 卷排序：127

文摘

Three different series of novel indolin-2-one-based sulfonamides were synthesized. Inhibitory activity of such sulfonamides was evaluated toward hCA I, II, IV and VII. 8, 3c and 6a-c emerged as single-digit nanomolar CA II inhibitors (5.9–9.4 nM). Molecular docking studies were carried out for some compounds within the hCA II active site.