Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 83, Issue -, Pages 674-684Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.06.076
Keywords
Carbamate; Methylseleno; Cytotoxicity; Apoptosis; Cell cycle arrest
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Funding
- Ministerio de Educacion y Ciencia, Spain [SAF 2009-07744]
- CAN Foundation [12,566]
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A series of new aliphatic, aromatic and heteroaromatic carbamate derivatives containing a methylseleno moiety were synthesized and evaluated in vitro for their cytotoxic activity against a panel of human cell lines including CCRF-CEM (lymphoblastic leukaemia), K-562 (lymphocytic leukaemia), HT-29 (colon carcinoma), HTB-54 (lung carcinoma), PC-3 (prostate carcinoma), MCF-7 (breast adenocarcinoma), 184B5 (non-malignant, mammary gland derived) and BEAS-2B (non-malignant, derived from bronchial epithelium). Most of the compounds are highly cytotoxic with GI(50) values below 10 mu M in every tested tumour cell line. Based on its cytotoxic parameters, selectivity index and ADME profile, the biological activity of compound 2, the propyl derivative, was further analysed in CCRF-CEM and HTB-54 cells. Results showed that this compound is able to induce apoptosis in a time- and dose-dependent manner. Involvement of caspases in cell death induction by 2 was detected. Besides, compound 2 was also able to induce cell cycle arrest at G(0)/G(1) in CCRF-CEM cells and at G(2)/M in HTB-54 cells. (C) 2014 Elsevier Masson SAS. All rights reserved.
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