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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 μM 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.

Original publication

DOI

10.1016/j.ejmech.2016.02.042

Type

Journal article

Journal

Eur J Med Chem

Publication Date

04/05/2016

Volume

113

Pages

134 - 144

Keywords

Apoptosis, Cytotoxicity, Selenium, Selenourea, Antineoplastic Agents, Apoptosis, Cell Proliferation, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, Humans, Molecular Structure, Organoselenium Compounds, Structure-Activity Relationship, Thiourea, Tumor Cells, Cultured, Urea