91桃色

Abstract

The pyrazole scaffold represents a common motif in many pharmaceutical active and remarkable compounds demonstrating a wide range of pharmacological activities; the most important activities are the anti-inflammatory, the antibacterialantifungal, the hypoglycemic, the anti-hyperlipidemic, the inhibition of cyclooxigenase-2, p38 MAP kinase and CDK2/Cyclin A, and the antiangiogenic. In the present work we are aiming to synthesis novel pyrazole derivatives together with their antitumor evaluations. the reaction of cyanoacetylhydrazine with chloroacetylchloride gave the N-acyl derivative 3. The the latter underwent ready cyclization in sodium ethoxide to give the pyrazole derivative 4 which was the key compound for the synthesis of thiophene, thieno[2,3-b]pridine and thiazole derivatives. The cytotoxicity of the newly synthesized products towards against three human tumor cells lines namely breast adenocarcinoma (MCF 7), non-small cell lung cancer (NCI-H460) and CNS cancer (SF-268) and some of these compounds were found to exhibit much higher inhibitory effects towards the three tumor cell lines than the reference doxorubicin.

Biography

Rafat Mohareb has completed his Ph. D at the age of 26 years from Cairo University. He got full Professer in 1994, participating with International fellows foundations like: the Alexander von Humboldt foundation, Full bright and the Arab-fund Foundation for Social and economic developments. He was published around 125 papers in the field of Pharmaceutical Chemistry.