RESUMEN
The propargyl alcohol on reaction with alkylazides under Sharpless conditions through click chemistry concept gave exclusively 1,4-disubstituted triazoles 2. The compounds 2 were oxidized to aldehydes 3 followed by reaction with aniline resulted Schiff's bases 4. The compounds 4 was further reacted with various aldehydes having α-hydrogen using molecular iodine as a catalyst and obtained 2-alkyl triazole-3-alkyl substituted quinoline derivatives 5. All the final compounds were screened against four human cancer cell lines (THP-1, Colo205, U937 & HeLa) and promising compounds have been identified.
Asunto(s)
Quinolinas/síntesis química , Quinolinas/farmacología , Triazoles/síntesis química , Triazoles/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Antineoplásicos/farmacología , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Células HeLa , Humanos , Quinolinas/química , Triazoles/química , Células U937RESUMEN
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 U(937), THP-1 and Colo205. The promising compounds 5b and 5e have been identified.