Multicomponent synthesis and anticancer activity studies of novel 6-(Trifluoromethyl)-1, 2, 3, 4-tetrahydropyrimidine-5-carboxylate derivatives

Abstract

A series of novel 6-(trifluoromethyl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate derivatives were obtained in good yields from ethyl 4,4,4-trifluoro-3-oxobutanoate, urea, and aryl aldehyde via Biginelli multicomponent reaction. All the corresponding products 4a–4p were examined against four human cancer cell lines (A549, HepG2, COLO205 and DU145) and compounds 4e, 4i, and 4 m which showed promising anticancer activity have been identified.

Graphical Abstract

Keywords:

• 6-(trifluoromethyl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate
• anticancer activity
• Biginelli condensationIntroduction

Additional information

Funding

The authors acknowledge the financial support of National Natural Science Foundation of China [No. 21676129], Jiangsu University scientific research funding [13JD062], and Jiangsu Postdoctoral Foundation [1601034B].