| 摘要 |
The invention relates to certain derivatives of mitomycins A and C having good anti-neo-plastic properties and low bone marrow and overall toxicity comprising: <IMG> wherein, n is 0 or 1; Y is selected from the group consisting of glucopyranosyl, galactopyranosyl, mannopyranosyl, xylopyranosyl, cellobiosyl, lactosyl, glucofuranosyl, maltosyl, and 1,3cyclohexanediol-2-yl or the hydroxyl-protected acetate derivatives thereof; R is hydrogen; R1 is hydrogen, C1-C4 alkyl or C1-C4 allyl substituted by phenyl, hydroxyphenyl,indolyl, mercapto, C1-C4 allylthio, hydroxy, carboxy, amino, guanidino, inidazole or carbamyl; or R and R1 form a five or six membered ring containing nitrogen; or <IMG> wherein, n, Y, R and R1 are the same as above; and 2 R2 is NH2 or CH3O-; or <IMG> wherein, R2 is as defined above; and R3 is a 3-cyano-4-morpholinyl-2-deoxypyranosyl saccharide or a 4-morpholinyl-2-deoxypyranosyl saccharide; and to methods for the preparation and use of the mitomycin derivatives.
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