Document Detail

Synthesis and in vitro Anticancer Activities of some Selenadiazole Derivatives.
MedLine Citation:
PMID:  21110339     Owner:  NLM     Status:  In-Data-Review    
A novel series of fourteen substituted selenadiazoles has been synthesized and the compounds tested for their in vitro antiproliferative and cytotoxic activities. The tests were carried out against leukemia (CCRF-CEM), colon (HT-29), lung (HTB-54), and breast (MCF-7) cancer cells. In order to assess the selectivity of the compounds under investigation the assays were also carried out on two non-tumoral lines - one mammary (184B5) and one bronchial epithelium (BEAS-2B) cell line. Assay-based antiproliferative activity studies revealed that seven derivatives (2a, 2c, 2e, 2f, 2g, 3a, and 3b) exhibited good activity against MCF-7 cells: for instance, 2c and 2f inhibited cell growth with nanomolar GI(50) values. Compound 2f had a better antitumoral profile than vinorelbine and paclitaxel, two drugs that are used as first-line treatments in advanced, recurrent, and/or metastatic cancer. In the other cell lines the compounds showed moderate activity or were inactive - with the exception of 2a, which was also found to have antiproliferative activity. Modulation of the cell cycle and apoptotic effects of active compounds were further evaluated in MCF-7 cells. Of these, 6-bromo[1,2,5]selenadiazolo[3,4-b]pyridine (2a) was the most active, with an apoptogenic effect 3.9 times higher than that of camptothecin, which was used as a positive control. Compound 2a also provoked cell cycle arrest with a significant decrease in the G(0)/G(1) phase cell population and an increase in S and G(2)/M cells, thus suggesting mitotic arrest prior to metaphase.
Daniel Plano; Esther Moreno; María Font; Ignacio Encío; Juan Antonio Palop; Carmen Sanmartín
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Archiv der Pharmazie     Volume:  343     ISSN:  1521-4184     ISO Abbreviation:  Arch. Pharm. (Weinheim)     Publication Date:  2010 Nov 
Date Detail:
Created Date:  2010-11-29     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0330167     Medline TA:  Arch Pharm (Weinheim)     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  680-91     Citation Subset:  IM    
Sección de Síntesis, Departamento de Química Orgánica y Farmacéutica, University of Navarra, Pamplona, Spain.
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