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

作者：Alcolea Veronica; Plano Daniel; Karelia Deepkamal N; Antonio Palop Juan; Amin Shantu; Sanmartin Carmen; Sharma Arun K^*

来源：European Journal of Medicinal Chemistry, 2016, 113: 134-144.

DOI：10.1016/j.ejmech.2016.02.042

• Selenium
• Selenourea
• Cytotoxicity
• Apoptosis

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 mu M 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.

• 出版日期2016-5-4