Anticancer Activities of Some New Synthesized Thiazolo[3,2-a]Pyrido[4,3-d]Pyrimidine Derivatives

Abstract

Problem statement: This study describes the synthesis and anticancer activities of a new series of thiazolo[3,2-a]pyrimidines derivatives (2-7) using 3,5-bisarylmethylene-1-methyl-4- piperidone and 4-aryl-8-arylmethelene-6-methylpyrido[4,3-d]pyrimidine-2(1H)thiones as a starting materials. Approach: The antitumor activities of the newly synthesized compounds 4-7 were evaluated utilizing 60 different human tumor cell lines, representing leukemia, melanoma, lung, colon, brain, ovary, breast and prostate as well as kidney. Results: Some of the tested compounds exhibited better in vitro antitumor activities at low concentration (log10 GI₅₀ = -4.7) against the used human tumor cell lines. Conclusion: From the obtained results, we can conclude that pyrimidine moieties fused to N-methylpipredine ring are essential for antitumor activities. In the present work, we can suggest that the anticancer activity is due to the presence of nitrogen heterocyclic rings and the presence of sulfur atom generally enhancing the activity.