RESUMEN
A series of novel 1,2,4-triazole derivatives incorporating benzisoselenazolone scaffold were designed, synthesized and evaluated for their in vitro antiproliferative activities against human cancer cell lines SMMC-7721, Hela, A549, and normal cell lines L929 by CCK-8 assay. The preliminary bioassay results demonstrated that most of the tested compounds 3a-3n exhibited antiproliferation with different degrees, and some compounds showed better effects than positive controls ethaselen and 5-fluorouracil (5-FU) against various cancer cell lines. Among these compounds, compounds 3b and 3c displayed highly effective biological activities against SMMC-7721cells with IC50 values of 6.02 and 6.01 µM, respectively. Compound 3n showed significant antiproliferative activities against Hela cells with IC50 value of 3.94 µM. Compound 3n exhibited the best inhibitory effect against A549 cells with IC50 value 9.14 µM. Furthermore, most of the tested compounds showed weak cytotoxic effect against the normal cell lines L929. The pharmacological results suggest that the substituent groups are vital for improving the potency and selectivity of this class of compounds.
Asunto(s)
Antineoplásicos/síntesis química , Triazoles/química , Antineoplásicos/química , Antineoplásicos/farmacología , Compuestos Bicíclicos Heterocíclicos con Puentes/química , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Ensayos de Selección de Medicamentos Antitumorales , Fluorouracilo/farmacología , Células HeLa , Humanos , Compuestos de Organoselenio/química , Relación Estructura-Actividad , Triazoles/síntesis química , Triazoles/farmacologíaRESUMEN
A series of novel nonsymmetrical disulfides bearing 1,3,4-oxadiazole moiety were designed, synthesized and evaluated for their in vitro antiproliferative activities against SMMC-7721, Hela and A549 human cancer cell lines by CCK-8 assay. The preliminary bioassay results demonstrated that all tested compounds 7a-7o exhibited antiproliferation with different degrees, and some compounds showed better effects than positive control 5-fluorouracil against various cancer cell lines. Among these compounds, compound 7j showed significant antiproliferative activity against SMMC-7721 cells with IC50 value of 3.40µM. Compound 7a displayed highly effective biological activity against Hela cells with IC50 value of 4.26µM. Compound 7g exhibited the best inhibitory effect against A549 cells with IC50 value of 6.26µM.