Amido/ureidosubstituted benzenesulfonamides-isatin conjugates as low nanomolar/subnanomolar inhibitors of the tumor-associated carbonic anhydrase isoform XII
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- 作者：Wagdy M. Eldehnaa ; wagdy2000@gmail.com" class="auth_mail" title="E-mail the corresponding author ; Mohamed Faresa ; Mariangela Cerusob ; Hazem A. Ghabbourc ; Sahar M. Abou-Serid ; Hatem A. Abdel-Azizc ; e ; Dalal A. Abou El Ellaf ; Claudiu T. Supuranb ; g ; claudiu.supuran@unifi.it" class="auth_mail" title="E-mail the corresponding author
- 关键词：Carbonic anhydrase ; Tumor-associated isoforms ; Amido/ureido sulfonamides ; Isatin
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：3 March 2016
- 年：2016
- 卷：110
- 期：Complete
- 页码：259-266
- 全文大小：600 K
文摘
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Different sulfonamides incorporating amido or ureido linkers were synthesized.
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Inhibitory activity of these sulfonamides was evaluated toward hCA I, II, IX and XII.
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9, 6b-g, 10c and 10e displayed outstanding potency against CA XII (KI: 0.47–0.71 nM).
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Other derivatives emerged as single-digit nanomolar CA XII inhibitors (1.17–2.83 nM).