Synthetic studies on quinocarcin and its related compounds. 5. Synthesis and antitumor activity of various structural types of quinocarcin congeners

Article abstract of DOI:10.1016/S0040-4020(01)80645-1

The antitumor activity of various structural types of quinocarcin congeners which had been previously prepared in the course of our synthetic studies or were originally synthesized by employing novel synthetic schemes, was primarily evaluated by in vitro cytotoxicity assay against P388 murine leukemia cells. Several compounds exhibiting prominent cytotoxicity were selected, and further subjected to in vitro cytotoxicity assay against HeLa S3 cells and to in vivo antitumor activity assay against P388 murine leukemia. These studies obviously disclosed novel aspects of the structure-activity relationships of quinocarcin congeners.