Add time:08/25/2019         Source:sciencedirect.com

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.

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