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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 l ines, 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 concent ration (log10 GI 50 = -4.7) against the used human tumor cell lines. Conclusion: From the obtained results, we can conclude that py rimidine moieties fused to N-methylpipredine ring are essential for a ntitumor 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 act ivity. |
