الفهرس 
IntroductionOnly 14 pages are availabe for public view
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Abstract
Objectives: The present study aimed to design, synthesis and biological evaluation of new thiazoles, thiazolopyrimidines and dithiazolopyrimidinones to reach an active antitumor agent with potentiated activity and selectivity toward cancerous cells. Methods: Compounds 123–144 were synthesized and tested for their in vitro antitumor activity against liver HepG2, colorectal HCT-116 and breast MCF-7, using standard MTT assay. The in vitro active antitumor analogs were assessed for in vivo antitumor efficacy over EAC in mice, cytotoxicity against normal cells and DNA-binding affinity. Also, The new analogs were studied for the prognosis of Lipinski’s rule of five, Veber’s criteria, toxicological properties, drug-likeness and drug score. Key findings: compounds 123, 133, 128 and 144h were proved to have prominent activity against the three tested cell lines. Conclusions: It could be concluded that compounds 123 and 133 are considered to be promising, selective and safe antitumor agents with decreased toxicity against normal cells, and with expected good oral absorption. Both compounds are predicted to show their biological activity through binding interaction with DNA.