Synthesis and Evaluation of Triazolyl Dihydropyrimidines as Potential Anticancer Agents


  •  Rajanna Ajumeera    
  •  Ganapathi Thipparapu    
  •  Shireesha Boyapati    
  •  Bharath Singh Padya    
  •  Vijayalaxmi Venkatesan    

Abstract

Novel N – 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 µM in MCF-7 cells and 41.50, 35.28, 32.06 µM 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.



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  • Issn(Print): 1916-9698
  • Issn(Onlne): 1916-9701
  • Started: 2009
  • Frequency: semiannual

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