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.
Highlights
Pyrimidines were nitrogen compounds, discovered in 1893 and are cyclic amines
The human breast cancer (MCF-7 &MDA MB231) cells were obtained from NCCS, Pune, India
After 24 h, the medium was replaced by fresh culture medium with IC50 concentrations of dihydropyrimidine derivatives (3a-f &4a-f)
Summary
Pyrimidines were nitrogen compounds, discovered in 1893 and are cyclic amines. It is known as m-diazone (or) 1, 3-diazine and got the recognition as parent nucleus of large group of heterocyclic compounds. The reduced pyrimidines i.e. dihydropyrimidines (DHPM) is an interesting heterocyclic ring, that was found to possess a vital role in numerous biological processes as it is the core nucleus of the endogenous molecules like nucleic acids, co-enzymes, several vitamins, purines and liposaccharides. It has been reported for various biological activities like antibacterial (Sangaraiah, et al, 2012), antifungal (Rami, et al, 2013), antiviral (Hockova, et al, 2003, Breault, et al, 2003), anticancer (Sosnicki, et al, 2014), antihypertensive (Chikhale, et al, 2009) with calcium channel blocking and dihydrofolate reductase inhibition. The toxicity of these derivatives was predicted by using in silico methods (Ganapathi et al, 2016)
Sign-in/Register to view highlights & summary 
Published Version (
Free)
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call