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

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-phe...

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Published in:Organic & biomolecular chemistry 2009-01, Vol.7 (22), p.4782-4788
Main Authors: Snégaroff, Katia, Lassagne, Frédéric, Bentabed-Ababsa, Ghenia, Nassar, Ekhlass, Ely, Sidaty Cheikh Sid, Hesse, Stéphanie, Perspicace, Enrico, Derdour, Aïcha, Mongin, Florence
Format: Article
Language:English
Subjects:
Antineoplastic Agents - pharmacology
Cadmium - pharmacology
Cell Death - drug effects
Cell Line, Tumor
Chemical Sciences
Doxorubicin - pharmacology
Drug Screening Assays, Antitumor
Halogenation - drug effects
Humans
Lithium - pharmacology
Organic chemistry
Pyrimidines - chemistry
Pyrimidines - pharmacology
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Summary: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.
ISSN:1477-0520
1477-0539
DOI:10.1039/b915274a