Design and Synthesis of Bis-Triazole-Linked Benzenesulfonamides as Selective Carbonic Anhydrase IX/XII Inhibitors with Chemosensitizing Activity

significantly enhanced the antiproliferative effects of azacitidine and sorafenib in breast and pancreatic cancer cells under both normoxic and hypoxic conditions. Molecular modeling and simulation studies further supported productive zinc coordination and stable active-site interactions. Overall, these findings highlight bis-triazole benzenesulfonamides as promising scaffolds for targeting hCA IX/XII-expressing tumors and improving chemosensitivity to conventional chemotherapeutics to overcome cancer resistance.

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Publication Details

Journal
Journal of Medicinal Chemistry
Published
2026-04-30
DOI
https://doi.org/10.1021/acs.jmedchem.6c00547
Primary Topic
Enzyme function and inhibition
Type
article
Field-Weighted Citation Impact
0.00

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article

Design and Synthesis of Bis-Triazole-Linked Benzenesulfonamides as Selective Carbonic Anhydrase IX/XII Inhibitors with Chemosensitizing Activity

Simone Giovannuzzi, Muhamad Mustafa, Ender Şi̇mşek, İ. Çelik et al.
Journal of Medicinal Chemistry
Enzyme function and inhibition
article

Design and Synthesis of Bis-Triazole-Linked Benzenesulfonamides as Selective Carbonic Anhydrase IX/XII Inhibitors with Chemosensitizing Activity

Simone Giovannuzzi, Muhamad Mustafa, Ender Şi̇mşek, İ. Çelik, Eslam Roshdy, Manabu Abe, Jean‐Yves Winum, Zeynep Betül Sarı, Ahmet Kilic, Özen Özensoy Güler, Alessio Nocentini, Claudiu T Supuran
article en

Abstract

significantly enhanced the antiproliferative effects of azacitidine and sorafenib in breast and pancreatic cancer cells under both normoxic and hypoxic conditions. Molecular modeling and simulation studies further supported productive zinc coordination and stable active-site interactions. Overall, these findings highlight bis-triazole benzenesulfonamides as promising scaffolds for targeting hCA IX/XII-expressing tumors and improving chemosensitivity to conventional chemotherapeutics to overcome cancer resistance.

Journal of Medicinal Chemistry
Hiroshima University (JP), École Nationale Supérieure de Chimie de Montpellier (FR), Centre National de la Recherche Scientifique (FR), Université de Montpellier (FR), Education Training And Research (US), Medicina (PL), Institut des Biomolécules Max Mousseron (FR), Kindeva Drug Delivery (United States) (US), Ankara Yıldırım Beyazıt University (TR), University of Florence (IT), Erciyes University (TR), Minia University (EG)
Support for Pioneering Research Initiated by the Next Generation, Erciyes Üniversitesi, Core Research for Evolutional Science and Technology
Openalex Percentile: Top 13%
Enzyme function and inhibition
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