الفهرس 
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Abstract
Novel series of thiazolo[4,5-d]pyrimidine derivatives have been synthesized, identified and biologically evaluated for their anticancer activity. Cytotoxic activities of all the synthesized compounds were examined through the National Cancer Institute’s developmental therapeutics program – United States of America (NCI-DTP-USA). Compound 3 was found to have a potent and broad-spectrum cytotoxic action against NCI panel with GI50 mean graph midpoint (MG-MID) = 2.88µM. MTT assay was used to determine IC50 values of the most potent agent against HCT-116 and WI-38 cell lines; 5.33 µM ±0.69 and 21.69µM ±1.04, respectively. Flow cytometric analysis revealed that compound 3 triggered apoptosis and G2/M cell cycle arrest. The ability of compound 3 to inhibit CDK1 (Cyclin-Dependent Kinase 1)/Cyclin B complex was evaluated, and its IC50 value was 97nM ± 2.33. Moreover, according to the gene expression analysis, compound 3 up-regulated p53, BAX, cytochrome C, caspase-3, caspase-8 and caspase-9 and down-regulated Bcl-2. In conclusion, compound 3 caused G2/M cell cycle arrest and induced apoptosis through the intrinsic pathway in a p53 dependent manner.