Possible chemical mechanisms underlying the antitumor activity of S-deoxyleinamycin

Though less potent than the parent natural product leinamycin, S-deoxyleinamycin displays activity against human cancer cell lines that is comparable to many clinically used agents. The results reported here suggest that the 1,2-dithiolan-3-one heterocycle found in S-deoxyleinamycin reacts with thiols to generate a persulfide intermediate (RSS−) that could deliver biologically active polysulfides, hydrogen sulfide, and reactive oxygen species (O2-, H2O2, and HO) to the interior of cells.

Though less potent than the parent natural product leinamycin, S-deoxyleinamycin displays activity against human cancer cell lines that is comparable to many clinically used agents. The 1,2-dithiolan-3-one heterocycle found in S-deoxyleinamycin may react with thiols to generate a persulfide intermediate (RSS−) that delivers biologically active polysulfides, hydrogen sulfide, and reactive oxygen species (O2-, H2O2, and HO) to the interior of cells.Figure optionsDownload as PowerPoint slide