Design, Synthesis And Screening Of The Derivatives Of The Compound Z24 As The Inhibitor Of Bcl-2 Protein

Despite the progress in basic and clinic medical sciences, cancer is still the second most frequent cause of death in the world. Traditional treatments of cancer often have strong side effects. Recently, the studied in oncology revealed that apoptosis was involved in tumorgenesis and multi-drug resistance in cancer treatment. The findings indicate that blocking of the apoptosis-inducing pathway could be another mechanism for multi-drug resistance (MDR). The regulation of apoptosis has been become a novel target for anticancer drug design.Bcl-2 protein, a bcl-2 gene product, is a 25KD a membrane protein that prevents cell apoptosis is overexpressed in many human cancers. Bcl-2's over-expression is associated with tumor development or progression and resistance to chemo- and radiotherapy. Because the bcl-2 gene is only over-expressed in tumor cells and its function is not necessary in normal cells, the bcl-2 inhibitor may have no or lower toxic side effect on normal cells.Z24 is a specific and effective inhibitor of the Bcl-2 protein. The results, in vitro and in vivo, showed that Z24 had good effect of...