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Paper

Org. Biomol. Chem., 2009, 7, 4782 - 4788, DOI: 10.1039/b915274a

Direct metallation of thienopyrimidines using a mixed lithium–cadmium base and antitumor activity of functionalized derivatives

Katia Snégaroff, Frédéric Lassagne, Ghenia Bentabed-Ababsa, Ekhlass Nassar, Sidaty Cheikh Sid Ely, Stéphanie Hesse, Enrico Perspicace, Aïcha Derdour and Florence Mongin

A series of thieno[2,3-d]- and thieno[3,2-d]pyrimidines have been easily synthesized using as key step a deproto-cadmiation–trapping sequence. Some of the compounds thus synthesized were screened for anticancer (cytotoxic) activities, and (S)-2-(6-iodo-2-phenylthieno[2,3-d]pyrimidin-4-ylamino)-3-phenylpropanoic acid proved to have a significant activity towards liver, human breast and cervix carcinoma cell lines.

Graphical abstract image for this article (ID: b915274a)