In Vitro and In Vivo Anti-Breast Cancer Activities of Some Newly Synthesized 5-(thiophen-2-yl)thieno-[2,3-d]pyrimidin-4-one Candidates.

In this study, some of new thiophenyl thienopyrimidinone derivatives - were prepared and tested as anti-cancer agents by using thiophenyl thieno[2,3-d]pyrimidinone derivative as a starting material, which was prepared from cyclization of ethyl ester derivative with formamide. Treatment of with ethyl- chloroacetate gave thienopyrimidinone -ethylacetate , which was reacted with hydrazine hydrate or anthranilic acid to afford acetohydrazide and benzo[d][1,]oxazin-4-one respectively. Condensation of with aromatic aldehydes or phenylisothiocyanate yielded Schiff base derivatives , and thiosemicarbazise , which were treated with 2-mercaptoacetic acid or chloroacetic acid to give the corresponding thiazolidinones , and phenylimino-thiazolidinone , respectively. Treatment of with ethylacetoacetate or acetic acid/acetic anhydride gave pyrazole and acetyl acetohydrazide derivatives, respectively. The latter compound was reacted with ethyl cycno-acetate or malononitrile to give and , respectively. In this work, we have studied the anti-cancer activity of the synthesized thienopyrimidinone derivatives against MCF-7 and MCF-10A cancer cells. Furthermore, in vivo experiments showed that the synthesized compounds significantly reduced tumor growth up to the 8 day of treatment in comparison to control animal models. Additionally, the synthesized derivatives showed potential inhibitory effects against pim-1 kinase activities.