ACS medicinal chemistry letters · 2024
Novel 2,4-Dichloro-5-sulfamoylbenzoic Acid Oxime Esters: First Studies as Potential Human Carbonic Anhydrase Inhibitors.
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Kilbile Jaydeo T, Sapkal Suryakant B, Renzi Gioele, D'Agostino Ilaria, Cutarella Luigi, Mori Mattia, De Filippis Barbara, Islam Imadul, Massardi Maria Luisa, Somenza Elena, Ronca Roberto, Tamboli Yasinalli, Carta Fabrizio, Supuran Claudiu T
Аннотация
In this study, a focused library of oxime ester derivatives of 2,4-dichloro-5-sulfamoylbenzoic acid (lasamide) containing Schiff bases was synthesized and tested in vitro for their ability to inhibit the cytosolic human carbonic anhydrases (hCAs) I and II, as well as the transmembrane and tumor-associated IX and XII isoforms. As a result, we obtained a first line of knowledge on lasamide derivatives potentially useful for development as CA inhibitors (CAIs). In particular, we focused our attention on the derivative 11, which was selective toward hCAs IX and XII over the cytosolic isoenzymes. An in silico study was conducted to assess the binding mode of 11 within hCAs IX and XII. Also, antiproliferative assays highlighted promising derivatives. The data obtained in this study are currently in use for the development of better-performing compounds on the tumor-associated isoforms.