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Eur J Med Chem. 2010 Dec;45(12):5732-8. doi: 10.1016/j.ejmech.2010.09.030. Epub 2010 Sep 17.

Novel 6-[(hetero)arylamino]thieno[3,2-b]pyridines: synthesis and antitumoral activities.

Author information

1
Centro de Química, Universidade do Minho, Campus de Gualtar, 4710-057 Braga, Portugal. mjrpq@quimica.uminho.pt

Abstract

Several novel 6-[(hetero)arylamino]thieno[3,2-b]pyridines were prepared by palladium-catalyzed C-N Buchwald-Hartwig coupling of the methyl 3-amino-6-bromothieno[3,2-b]pyridine-2-carboxylate with aryl and heteroarylamines, using different reaction conditions. The antitumoral activity of the di(hetero)arylamines obtained was evaluated against three representative human tumor cell lines, namely breast adenocarcinoma (MCF-7), melanoma (A375-C5), and non-small cell lung cancer (NCI-H460) and some structure-activity relationships were established within each series. The most promising compounds were shown to be a benzothiazole derivative with GI50 3.5-6.9 μM followed by an indole derivative with GI50 13-21 μM.

PMID:
20934235
DOI:
10.1016/j.ejmech.2010.09.030
[Indexed for MEDLINE]

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