Pyrazolylbenzo[d]imidazoles as new potent and selective inhibitors of carbonic anhydrase isoforms hCA IX and XII
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- 作者：Satish Kumara ; Mariangela Cerusob ; Tiziano Tuccinardic ; Claudiu T. Supuranb ; claudiu.supuran@unifi.it" class="auth_mail" title="E-mail the corresponding author ; Pawan K. Sharmaa ; pksharma@kuk.ac.in" class="auth_mail" title="E-mail the corresponding author
- 关键词：Carbonic anhydrase isoforms ; Pyrazolylbenzo[d]imidazoles ; Acetazolamide ; Inhibition constant (Ki)
- 刊名：Bioorganic & Medicinal Chemistry
- 出版年：2016
- 出版时间：1 July 2016
- 年：2016
- 卷：24
- 期：13
- 页码：2907-2913
- 全文大小：1042 K
文摘
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12 novel pyrazolylbenzo[d]imidazoles were designed and synthesized.
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Their inhibition potential was evaluated against hCA I, II, IX and XII.
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Compounds having sulfonamide moiety were better inhibitors with poor selectivity.
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Selectivity against tumor isoforms hCA IX abd XII enhanced on removing sulfonamide.
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Inhibition results were promising as compared to antitumor drug acetazolamide.