Synthesis And Anticancer Activity Study Of Bcl-2 Protein Inhibitors, And Synthesis Of An Antitubercular Nudeoside Compound

Apoptosis is essential for normal cell development, host defense and suppression of concogenesis. Meanwhile, apoptosis is aslo one of the major mechanisms for cell death in response to cancer therapies. Its dysregulation has been implicated in cancer and many other human diseases. It was reported that antiapoptic Bcl-2 proteins are significantly overexpressed in a variety of human cancer cells. Bcl-2 proteins therefore are emerging as attractive therapeutic target for cancer chemotherapy,and their inhibitors mignt be potential anticancer drug.In order to develop novel small molecule inhibitors of Bcl-2 proteins, the following work had been carried out: a total of 31 novel target compounds were synthesized based on WL-276, a reported Bcl-2 protein antagonist, and all the target molecules were indentified by 1HNMR,13CNMR,HRMS. The anticancer activities of the synthesized target compounds were evaluated on the HL-60 cell lines with MTT assay. Seven compound(s3b-1,3b-3,3a-3,3c-3,3f-3,3m-1 and WL-V13)display effective inhibition on HL-60 cell line.