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.

1,2-Benzisothiazole Derivatives Bearing 4-, 5-, or 6-Alkyl/arylcarboxamide Moieties Inhibit Carbonic Anhydrase Isoform IX (CAIX) and Cell Proliferation under Hypoxic Conditions

SARTINI, STEFANIA;MARINI, ANNA MARIA;SIMORINI, FRANCESCA;TALIANI, SABRINA;SALERNO, SILVIA;ORLANDI, PAOLA;FIORAVANTI, ANNA;DA SETTIMO PASSETTI, FEDERICO;BOCCI, GUIDO
Penultimo
;
LA MOTTA, CONCETTINA
Ultimo
2016

Abstract

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.
Coviello, Vito; Marchi, Beatrice; Sartini, Stefania; Quattrini, Luca; Marini, ANNA MARIA; Simorini, Francesca; Taliani, Sabrina; Salerno, Silvia; Orlandi, Paola; Fioravanti, Anna; Desidero, Teresa Di; Vullo, Daniela; DA SETTIMO PASSETTI, Federico; Supuran, Claudiu T; Bocci, Guido; LA MOTTA, Concettina
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/802851
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