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Bioorg Chem ; 97: 103677, 2020 04.
Artículo en Inglés | MEDLINE | ID: mdl-32120075

RESUMEN

A series of cycloalkanecarboxamide-containing sulfonate and sulfamate derivatives were prepared, and their antiproliferative activity was tested against NCI-60 cancer cell lines panel. Compound 1f possessing cyclohexyl and p-(tert-butyl)benzenesulfonate moieties was the most active among all the target compounds. It exerted broad-spectrum anticancer activity against all the nine cancer types involved in the NCI-60 panel. Additionally, compound 1g containing cyclohexyl and p-fluorobenzenesulfonate moieties was the most potent against HT29 colon cancer cell line (IC50 = 4.73 µM) with selectivity index more than 4.23 towards HT29 than normal fibroblasts. It exerts its antiproliferative activity against HT29 through the induction of apoptosis (increasing caspase 3/7 activity) but not necrosis. Structure-activity relationship studies are presented in detail.


Asunto(s)
Antineoplásicos/química , Antineoplásicos/farmacología , Proliferación Celular/efectos de los fármacos , Cicloparafinas/química , Cicloparafinas/farmacología , Apoptosis/efectos de los fármacos , Línea Celular Tumoral , Neoplasias del Colon/tratamiento farmacológico , Ensayos de Selección de Medicamentos Antitumorales , Células HT29 , Humanos , Relación Estructura-Actividad , Ácidos Sulfónicos/química , Ácidos Sulfónicos/farmacología
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