Mitomycin derivatives having reduced bone marrow toxicity,...

Details Mitomycin derivatives having reduced bone marrow toxicity,... Mitomycin derivatives having reduced bone marrow toxicity,...

C - Chemistry, Metallurgy

07

D

167/180, 260/228

C07D 487/14 (2006.01) A61K 31/70 (2006.01) C07H 5/04 (2006.01)

Patent

CA 1327037

ABSTRACT 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: Image wherein, n is 0 or 1; Y is selected from the group consisting of glucopyranosyl, galactopyranosyl, mannopyranosyl, xylopyranosyl, cellobiosyl, lactosyl, glucofuranosyl, maltosyl, and 1,3- cyclohexanediol-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 Image wherein, n, Y, R and R1 are the same as above; and 2 R2 is NH2 or CH3O-; or Image 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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