abstract |
A compound of the structure <IMAGE> where R1, R2, and R3 are each, independently, hydrogen or <IMAGE> with the proviso that R1, R2, and R3 are not all hydrogen; R4 is -(CH2)mX(CH2)nCO2R5 or <IMAGE> R5 and R6 are each, independently, alkyl, aralkyl, or phenyl which is optionally mono-, di-, or tri-substituted with a substituent selected from alkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, amino, or a carboxylic acid; X is <IMAGE> R7 and R8 are each, independently, hydrogen or alkyl; Y is CH or N; m is 0-4; n is 0-4; with the proviso that m and n are not both 0 when X is O or S; or a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppresive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases, and diseases of inflammation, by virtue of its antitumor activity useful in treating tumors, and by virtue of its antifungal activity is useful in treating fungal infections. |