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-phenylpropanoic acid proved to have a significant activity towards liver, human breast and cervix carcinoma cell lines.
Snégaroff
Katia
K
Chimie et Photonique Moléculaires, UMR 6510 CNRS, Université de Rennes 1, Bâtiment 10A, Case 1003, Campus Scientifique de Beaulieu, 35042, Rennes, France.
Lassagne
Frédéric
F
Bentabed-Ababsa
Ghenia
G
Nassar
Ekhlass
E
Ely
Sidaty Cheikh Sid
SC
Hesse
Stéphanie
S
Perspicace
Enrico
E
Derdour
Aïcha
A
Mongin
Florence
F
D000970:Antineoplastic Agents / Q000494:pharmacology*; D002104:Cadmium / Q000494:pharmacology*; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D004317:Doxorubicin / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D054879:Halogenation / Q000187:drug effects; D006801:Humans; D008094:Lithium / Q000494:pharmacology*; D011743:Pyrimidines / Q000737:chemistry / Q000494:pharmacology*
D000970:Antineoplastic Agents; D011743:Pyrimidines; C476003:thienopyrimidine; D002104:Cadmium; D004317:Doxorubicin; D008094:Lithium