A series of disubstituted selenazole derivatives was synthetized and evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors against the human (h) isoforms hCA I, II, IV, VA, VB and IX, involved in a variety of diseases including glaucoma, retinitis pigmentosa, epilepsy, arthritis and tumors. The investigated compounds showed potent inhibition against the tumor-associated transmembrane hCA IX, with KIs in the subnanomolar – low nanomolar range, and were evaluated for their effects on cell viability against the human prostate (PC3) and breast (MDA-MB-231) cancer cell lines, showing effective anti-tumor activity. These selenazoles are interesting leads for the development of new, isoform-selective CA IX inhibitors.

Discovery of new 2, 5-disubstituted 1,3-selenazoles as selective human carbonic anhydrase IX inhibitors with potent anti-tumor activity / Angeli, Andrea; Trallori, Elena; Ferraroni, Marta; Di Cesare Mannelli, Lorenzo; Ghelardini, Carla; Supuran, Claudiu T.*. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 157:(2018), pp. 1214-1222. [10.1016/j.ejmech.2018.08.096]

Discovery of new 2, 5-disubstituted 1,3-selenazoles as selective human carbonic anhydrase IX inhibitors with potent anti-tumor activity

Angeli, Andrea;Trallori, Elena;Ferraroni, Marta;Di Cesare Mannelli, Lorenzo;Ghelardini, Carla;Supuran, Claudiu T.
2018

Abstract

A series of disubstituted selenazole derivatives was synthetized and evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors against the human (h) isoforms hCA I, II, IV, VA, VB and IX, involved in a variety of diseases including glaucoma, retinitis pigmentosa, epilepsy, arthritis and tumors. The investigated compounds showed potent inhibition against the tumor-associated transmembrane hCA IX, with KIs in the subnanomolar – low nanomolar range, and were evaluated for their effects on cell viability against the human prostate (PC3) and breast (MDA-MB-231) cancer cell lines, showing effective anti-tumor activity. These selenazoles are interesting leads for the development of new, isoform-selective CA IX inhibitors.
2018
157
1214
1222
Angeli, Andrea; Trallori, Elena; Ferraroni, Marta; Di Cesare Mannelli, Lorenzo; Ghelardini, Carla; Supuran, Claudiu T.*
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1141018
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