Abstract
We are aiming in this work to synthesize target molecules not only possess antitumor activities but also kinase inhibitors. The target molecules were obtained from dimedone, which reacted with triethoxymethane to produce a product that is capable for many heterocyclization reactions to give fused pyrazole, thiophene and isoxazole derivatives. Compounds7b,7c,7d,9b,11,12c,12d,14b,16b,17c,17d,18c,18d, and18ewere the most cytotoxic compounds, their further tests toward the five tyrosine kinases c-Kit, Flt-3, VEGFR-2, EGFR, and PDGFR and Pim-1 kinase showed that compounds7b,7d,11,12c,14b,16b,17d,18d, and18ewere the most potent of the tested compounds toward the five tyrosine kinases and compounds7b,7d,14b,16b, and18ewere of the highest inhibitions toward Pim-1 kinase. PAINS the most cytotoxic compounds showed zero PAINS alert, therefore, these compounds can be used as useful drugs in the future.