Synthesis, structure–activity relationship of novel substituted 4H-chromen-1,2,3,4-tetrahydropyrimidine-5-carboxylates as potential anti-mycobacterial and anticancer agents

Series of 4H-chromen-1,2,3,4-tetrahydropyrimidine-5-carboxylate derivatives 7a–7zb, 8a–8d and 9a–9d were synthesized and screened for their in vitro anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv (MTB) and cytotoxicity against three human cancer cell lines including A549, SK-N-SH and HeLa. The results indicate that six compounds are more potent and 7za is most effective anti-mycobacterial derivative compared to the standard drugs Ethambutol and Ciprofloxacin. However, 12 compounds exhibited cytotoxicity against human neuroblastoma cell line; amongst them the compound 7v is most effective compared to the standard drug Doxorubicin. This is the first report assigning in vitro anti-mycobacterial, anticancer and structure–activity relationship for this new class of 4H-chromen-1,2,3,4-tetrahydropyrimidine-5-carboxylates.

Series of 4H-chromen-1,2,3,4-tetrahydropyrimidine-5-carboxylate derivatives were synthesized, screened for their anti-mycobacterial and anticancer activities, among them compound 7za is more potent anti-mycobacterial, 7v more potent anticancer agents compared to standard drugs and are being reported in this study for the first time to serve as a model compounds for design and development of therapeutic based anti-mycobacterial and anticancer activity.Figure optionsDownload as PowerPoint slide