1,2-Benzisothiazole Derivatives Bearing 4-, 5-, or 6-Alkyl/arylcarboxamide Moieties Inhibit Carbonic Anhydrase Isoform IX (CAIX) and Cell Proliferation under Hypoxic Conditions
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- 作者：Vito Coviello ; Beatrice Marchi ; Stefania Sartini ; Luca Quattrini ; Anna Maria Marini ; Francesca Simorini ; Sabrina Taliani ; Silvia Salerno ; Paola Orlandi ; Anna Fioravanti ; Teresa Di Desidero ; Daniela Vullo ; Federico Da Settimo ; Claudiu T. Supuran ; Guido Bocci ; Concettina La Motta
- 刊名：Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：July 14, 2016
- 年：2016
- 卷：59
- 期：13
- 页码：6547-6552
- 全文大小：298K
- 年卷期：0
- ISSN：1520-4804
文摘
Three novel series of 1,2-benzisothiazole derivatives have been developed as inhibitors of carbonic anhydrase isoform IX. Compounds 5c and 5j, tested in vitro on the human colon cell line HT-29, blocked the growth of cells cultured under chemically induced hypoxic conditions, displaying a specific activity against cancer cells characterized by CAIX up-regulation. Moreover, a synergistic activity of 5c with SN-38 (the active metabolite of irinotecan) and 5-fluorouracil on cell proliferation under hypoxic conditions was demonstrated.