The growing importance of functionalized aziridines in numreous organic biomolecules led us to develop syntheses of novel actinomycin D (AMD) analogues substituted with an aziridine. Reaction of 7-hydroxyactinomycin D with 2-(iodomethyl) aziridine produced the desired 7-(2-aziridinylmethoxy) actinomycin analogue. In an attempt to develop an alternate route to this analogue, 7-(2-azido-3-iodopropoxy) actinomycin was subjected to reduction ...