Synthesis And Bioactive Evaluation Of New 1,3,4-Oxadiazole Derivatives As Potential Anticancer Agents

Telomerase, which can promote endless telomeric synthesis that is essential for development of human tumors, is now widely acknowledged as a common Tumor Marker. Telomerase is usually highly expressed in a variety of tumor cells but not normal cells. On the other hand, tumor cells would die faster than normal cells when telomerase is chosen as therapeutic target for human cancer as they have shorter telomere.1,3,4-Oxadiazole has been reported to have many different biological activities such as anti-worms, anti-bactericidal, anti-cancer, anti-infammatory, and that is the reason it has been widely used in the area of medicine and pesticide. It can be easily metabolized in human body and the hydrogen bond can be formed so as to be used as an effective medical group.A series of 1,3,4-oxadiazole derivatives were synthesized to evaluate for antiproliferative activities against the human cancer cell line HepG-2, SGC-7901 and MCF-7 inhibitory activity. Biological evaluation indicated that compounds 5d and 5i were found to display potent antiproliferative activity. Moreover, docking simulations were performed to give the probable binding modes of these compounds into the telomerase active binding site of telomerase, which will support this result.