Synthesis and Evaluation of Triazolyl Dihydropyrimidines as Potential Anticancer Agents

Rajanna Ajumeera, Ganapathi Thipparapu, Shireesha Boyapati, Bharath Singh Padya and Vijayalaxmi Venkatesan

International Journal of Chemistry, 2018, vol. 10, issue 4, 18-27

Abstract: Novel N ¨C triazolyl 3(a-f) and O-triazolyl (4a-f) derivatives of 4, 6-diaryl-1, 4-dihydropyrimidines were synthesized through mannich reaction. All compounds were characterized by physical and spectral data. These compounds were screened for in vitro efficiency in human breast cancer cell (MCF-7&MDA-MB-231) lines and found to have very good anti-proliferative activity. Among all compounds of 4b, 3e, 4e endowed with lesser respective IC50 values of 31.94, 55.73, 55.03 ¦ÌM in MCF-7 cells and 41.50, 35.28, 32.06 ¦ÌM in MDA-MB 231 cells by MTT assay. In further studies, Compounds 4b, 3e, 4e were found to arrest cell growth at S phase in MCF-7 cells. In MDA-MB 231 cells, 4b, 4e were found to arrest the cells in S phase, and compound 3e found to arrest G2/M phase when compared to the standard drug tamoxifen, arrested S phase in MCF-7 cells and G0/G1 phase in MDA-MB 231 cells.

Keywords: dihydropyrimidines; triazoles; anticancer activity; cell cycle; breast cancer cells; MTT assay (search for similar items in EconPapers)
Date: 2018
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