Synthesis of novel alkyltriazole tagged pyrido[2,3-d]pyrimidine derivatives and their anticancer activity

A series of novel alkyltriazole tagged pyrido[2,3-d]pyrimidine derivatives 5 and 6 was prepared starting from 2,3-active functional pyridine 1via 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 U937, 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.Figure optionsDownload as PowerPoint slideHighlights
► 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.