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Synthesis of novel alkyltriazole tagged pyrido[2,3-d]pyrimidine derivatives and their anticancer activity
Ist Teil von
European journal of medicinal chemistry, 2011-08, Vol.46 (8), p.3462-3468
Ort / Verlag
Kidlington: Elsevier Masson SAS
Erscheinungsjahr
2011
Quelle
MEDLINE
Beschreibungen/Notizen
A series of novel alkyltriazole tagged pyrido[2,3-d]pyrimidine derivatives
5 and
6 was prepared starting from 2,3-active functional pyridine
1
via cyclization, propargylation followed by reaction with alkyl or perfluoroalkyl azides under Sharpless conditions. All the compounds
5 and
6 were screened for anticancer activity against three cancer cell lines such as U
937, THP-1 and Colo205. The promising compounds
5b and
5e have been identified.
A series of novel alkyltriazole tagged pyrido[2,3-d]pyrimidine derivatives
5 and
6 was prepared, screened for anticancer activity against three cancer cell lines and identified promising compounds
5b and
5e.
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► Sulphuric acid catalysed synthesis of novel pyrido[2,3-d]pyrimidine-4(3H)ones. ► Propargylation to obtain O- and N-propargylated pyrido[2,3-d]pyrimidines. ► Each isomer was reacted with alkyl azide under Sharpless conditions. ► Exclusively 1,4-disubstituted triazole tagged pyrido[2,3-d]pyrimidines formed. ► Final products screened for anticancer activity against three cancer cell lines.