A new antitumor agent: Methyl sulfonium perchlorate of echinomycin

Newly modified-echinomycin such as S-methylated sulfonium perchlorate of echinomycin (1), monosulfoxide (2), disulfoxide (3) and sulfone (4) have been prepared and evaluated for in vitro biological activities of cytotoxicity against P388, B16 and SNU-16 as well as in vivo antitumor activity against murine leukemia P388 and melanoma B16. Newly modified-echinomycin such as S-methylated sulfonium perchlorate of echinomycin (1),monosulfoxide (2), disulfoxide (3) and sulfone (4) have been prepared and evaluated for in vitro biological activities of cytotoxicity against P388, B16 and SNU-16 as well as in vivo antitumor activity against murine leukemia P388 and melanoma B16. Compound 1 showed highly as effective against murine leukemia and melanoma as 1 with broader range of therapeutic doses.