ARTÍCULO

Novel seleno- and thio-urea derivatives with potent in vitro activities against several cancer cell lines

Autores: Alcolea Devesa, Verónica; Plano Amatriain, Daniel; Karelia, D. N.; Palop Cubillo, Juan Antonio; Amin, S.; Sanmartín Grijalba, María del Carmen; Sharma, A. K.
Título de la revista: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN: 0223-5234
Volumen: 113
Páginas: 134 - 144
Fecha de publicación: 2016
Resumen:
A series of novel selenourea derivatives and corresponding thiourea analogs were synthesized and tested against a panel of six human cancer cell lines: melanoma (1205Lu), lung carcinoma (A549), prostatic carcinoma (DU145), colorectal carcinoma (HCT116), pancreatic epithelioid carcinoma (PANC-1) and pancreatic adenocarcinoma (BxPC3). In general, we found that the selenium-containing derivatives were more potent than their isosteric sulfur analogs. Four selenourea derivatives (1e, 1f, 1g and 1i) showed IC50 values below 10 mM in all of tested cell lines at 72 h. On the basis of its potent activity, compound 1g was selected for further biological evaluation in different colon cancer cell lines. Our results indicated that compound 1g induced apoptosis by caspase activation, along with inhibition of anti-apoptotic proteins.