Find in Library

In this study, some of new thiophenyl thienopyrimidinone derivatives <b>2</b>&#8722;<b>15</b> were prepared and tested as anti-cancer agents by using thiophenyl thieno[2,3-d]pyrimidinone derivative <b>2</b> as a starting material, which was prepared from cyclization of ethyl ester derivative <b>1</b> with formamide. Treatment of <b>2</b> with ethyl- chloroacetate gave thienopyrimidinone <i>N</i>-ethylacetate <b>3</b>, which was reacted with hydrazine hydrate or anthranilic acid to afford acetohydrazide <b>4</b> and benzo[d][1,³]oxazin-4-one <b>5,</b> respectively. Condensation of <b>4</b> with aromatic aldehydes or phenylisothiocyanate yielded Schiff base derivatives <b>6,7</b>, and thiosemicarbazise <b>10</b>, which were treated with 2-mercaptoacetic acid or chloroacetic acid to give the corresponding thiazolidinones <b>8</b>, <b>9,</b> and phenylimino-thiazolidinone <b>11</b>, respectively. Treatment of <b>4</b> with ethylacetoacetate or acetic acid/acetic anhydride gave pyrazole <b>12</b> and acetyl acetohydrazide <b>13</b> derivatives, respectively. The latter compound <b>13</b> was reacted with ethyl cycno-acetate or malononitrile to give <b>14</b> and <b>15</b>, 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^th day of treatment in comparison to control animal models. Additionally, the synthesized derivatives showed potential inhibitory effects against pim-1 kinase activities.