| abstract |
A compound of the structure <IMAGE> wherein R1 and R2 are each, independently, hydrogen, -CONHa-{{(CR3R4)m(-A-(CR5R6)n)p}q-B}r; -SO2R7; -SO3H; -CHR8O(CH2)tR9; or <IMAGE> R3, R4, R5, R6, and B are each, independently, hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, cycloalkyl, -OR10, -SR10, halogen, -CN, -NO2, -CF3, -COR10, -CO2R10, -CONHR10, -SO2R10, -OSO3R10, -NR10R11, -NHCOR10, -NHSO2R10, or Ar; X is =NOR12 or =NNR12R13; Y is O, =NOR12, or =NNR12R13; R7, R12, and R13 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, arylalkyl; R8, R9, R10, and R11 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, or Ar; A is -CH2-, -NR8-, -O-, -S-, -SO-, -SO2-, -PR8-, -CO-, -NHCO-, -NHSO-, or -P(O)(R8)-; Ar is aryl which may be optionally mono-, di-, or tri- substituted; <IMAGE> is a nitrogen containing heterocycle that may be saturated, unsaturated, or partially unsaturated, and may be optionally mono-, di-, or tri- substituted; a=0-1; m=0-6; n=0-6; p=0-1; q=0-1; r=1-2; and t=1-4; wherein R3, R4, R5, R6, A, B, m, n, p, and q are independent in each of the -CON-{{(CR3R4)m(-A-(CR5R6)n)p}q-B}r subunits when r=2; with the proviso that R1 and R2 are not both hydrogen, and further provided that if r=2, then a=0, and if r=1, then a=1; or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent. |