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.

Graphical abstractA 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 full-size imageDownload 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.