Insignificant anticancer activity of novel substituted pyrimidine derivatives

Abstract

Background: Pyrimidine and fused pyrimidine derivatives play an important role in
therapeutic strategies. It is known to be most prominent structures found in nucleic
acid, including uracil, thymine, cytosine, adenine, and guanine, which are fundamental
building blocks for deoxyribonucleic acid (DNA) and ribonucleic acid (RNA).
Materials and Methods: A series of 3-[2-amino-6-(substituted)-pyrimidin-4-yl]-6-
(substituted)-2H-chromen-2-one derivatives were prepared by reacting salicylaldehyde
with ethylacetoacetate in the presence of piperidine by Knoevenagel reaction as a
starting material. The chemical structures were confirmed by means of FTIR (Fourier
Transform InfraRed Spectrophotometer-8400S), 1H NMR, and elemental analysis. The
data of these synthesized compounds were submitted to National Institute of Health,
USA, under the drug discovery program of NCI (National Cancer Institute) and
screened for anticancer activity at a single high dose (10−5 M) in full NCI 60 cell lines.
Results: Unfortunately, the selected compounds have not shown any potent significant
anticancer activity in the NCI 60 cell line screening. Conclusion: The compound (T2)
found to be most efficient anticancer activity with selective influence on breast cancer
cell lines, especially on MCF7 cell line with a growth percentage of 33.63.