Design Synthesis And Activity Study Of Thioxo Thiazolidinone Compounds As Inhibitors Of Anti-apoptotic Bcl-2 Proteins

The anormal of cell apoptosis will lead to happen of many other human diseases include cancer. Bcl-2 family proteins have an important role in regulating apoptosis. Antiapoptotic Bcl-2 proteins are significantly overexplation in many different human cancer cells, for example, prostate cancer, pancreatic cancer, liver cancer and lung cancer. It suggested that anti-apoptotic Bcl-2 proteins have emerged as attractive targets for the development of anti-tumour agents. In this thesis, 39 BHI-1 ramifications of Bcl-2 protein inhibitors were synthesized, starting from L-Val, L-leu via a series of reactions. The structure of the target compounds were determined by 1H NMR, 13C NMR,IR and MS/ESI. The in vitro anticancer activitiy of the synthesized compounds were evaluated on the HL-60 cell lines using MTT assay method. Ten compounds inhibited the growth of HL-60 cell effectively, with IC50 values at micromolar level.