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Direct metallation of thienopyrimidines using a mixed lithium–cadmium base and antitumor activity of functionalized derivatives†
Katia Snégaroff,Frédéric Lassagne,Ekhlass Nassar,Sidaty Cheikh Sid Ely,Stéphanie Hesse,Enrico Perspicace,Aïcha Derdour,Florence Mongin
Organic & Biomolecular Chemistry Pub Date : 09/22/2009 00:00:00 , DOI:10.1039/B915274A
Abstract

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