Design, Sythesis And Antitumor Activity Evaluation In Vitro Of1,3,4-oxadiazole Derivatives

Cancer is a term for malignant category, is one of the world’s most difficultdiseases. The characteristics of cancer cells is unlimited, endless hyperplasia, makethe patient’s body nutrients are consumed largely.1,3,4-oxadiazole derivatives havebroad biological activity, especially the worlf known antitumor activity. Preliminaryscreening in vitro antitumor activity of derivatives with1,3,4-oxadiazole nucleus,becoming an urgent requirement to develop new, low toxicity, good selectiveanti-tumor drug.Based on the anti-tumor activity QSAR preliminary summary of derivatives with1,3,4-oxadiazole-2-thione nucleus,12new structure1,3,4-oxadiazole-2-thionederivatives have been designed and synthesised. By esterification, condensation,hydrazinolysis and cyclization, the target compounds were synthesized. And itschemical structure is confirmed by ESI-MS and1H NMR. The synthetic process oftarget compounds have been made detailed elaboration and discussion of the mattersneeding attention.By using the determined by MTT method of ImAtinib mesylate for positivecontrol, this paper makes a preliminary in vitro anti-proliferative activity evaluationof new compounds, which are anti-CML line K562, anti-hepatoma cell line Hep G2.Results show that the synthesized compounds showed weak antiproliferative activityof anti-CML line K562and anti-hepatoma cell line Hep G2. Antitumor activity of thetarget compounds exhibit selectivity for K562cells than Hep G2cells, providing animportant basis for further structural modification.