Preparation and Antitumor Activity of New Mitomycin A Analogues

Article abstract of DOI:10.1021/jm00384a028

A series of 26 mitomycin A analogues including 23 new ones was prepared by a variety of methods.The most useful methods were alkoxide exchange on mitomycin A and treatment of 7-hydroxymitosane with 3-substituted 1-phenyltriazenes.Many of the new analogues were superior to mitomycin C in the P388 leukemia assay and the more stringent subcutaneous B16 melanoma assay both in mice.Four of them gave long-term survivors in the latter assay.Quantitative correlations between log P and antitumor activity were not possible, but some guidelines for future analogue development are proposed.