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1.
Future Med Chem ; 15(2): 147-166, 2023 01.
Artículo en Inglés | MEDLINE | ID: mdl-36762576

RESUMEN

Background: Among the important key modulators of the tumor microenvironment and hypoxia is a family of enzymes named carbonic anhydrases. Herein, 11 novel sulfonamide-pyridine hybrids (2-12) were designed, synthesized and biologically evaluated for their potential use in targeting breast cancer. Methods & results: The para chloro derivative 7 reported the highest cytotoxic activity against the three breast cancer cell lines used. In addition, compound 7 was found to induce cell cycle arrest and autophagy as well as delaying wound healing. The IC50 of compound 7 against carbonic anhydrase IX was 253 ± 12 nM using dorzolamide HCl as control. Conclusion: This study encourages us to expand the designed library, where more sulfonamide derivatives would be synthesized and studied for their structure-activity relationships.


Asunto(s)
Neoplasias de la Mama , Femenino , Humanos , Antígenos de Neoplasias/metabolismo , Apoptosis , Neoplasias de la Mama/tratamiento farmacológico , Inhibidores de Anhidrasa Carbónica/farmacología , Inhibidores de Anhidrasa Carbónica/metabolismo , Anhidrasa Carbónica IX/antagonistas & inhibidores , Estructura Molecular , Piridinas/farmacología , Relación Estructura-Actividad , Sulfonamidas/farmacología , Microambiente Tumoral
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