Abstract: Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X2, R1, R2, R3, R6, R7, and R12 are each independently selected from the group consisting of H, OH, OR?, SH, SR?, SOR?, SO2R?, NO2, NH2, NHR?, N(R?)2, NHCOR?, NHSO2R?, CN, halogen, ?O, C(?O)H, C(?O)R?, CO2H, CO2R?, carboxyalkyl, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R? groups is independently selected from the group consisting of H, OH, SH, NO2, NH2, CN, halogen, ?O, C(?O)H, C(?O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups of R1 and R2, R2 and R3, R3 and R12, R12 and R6, or R6 and R7 may be joined into a carbocyclic or heterocyclic ring system.

Abstract: Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X2, R1, R2, R3, R6, R7, and R12 are each independently selected from the group consisting of H, OH, OR?, SH, SR?, SOR?, SO2R?, NO2, NH2, NHR?, N(R?)2, NHCOR?, NHSO2R?, CN, halogen, ?O, C(?O)H, C(?O)R?, CO2H, CO2R?, carboxyalkyl, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R? groups is independently selected from the group consisting of H, OH, SH, NO2, NH2, CN, halogen, ?O, C(?O)H, C(?O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups of R1 and R2, R2 and R3, R3 and R12, R12 and R6, or R6 and R7 may be joined into a carbocyclic or heterocyclic ring system.

Abstract: The invention provides variolin derivatives of formula (I), wherein: R1 and R2 are each independently selected from the group consisting of H, OH, OR, SH, SR, SOR, SO2R, NO2, NH2, NHR, N(R)2, NHCOR, N(COR)2, NHSO2R, CN, halogen, C(?O)H, C(?O)R, CO2H, CO2R, C1-C12 alkyl, C1-C12 haloalkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; and R3 is selected from the group consisting of H, OH and OMe; wherein the or each group R is independently selected from the group consisting of OH, C1-C12 alkyl, C1-C12 haloalkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted unsubstituted aralkyl, substituted or unsubstituted arylalkenyl and substituted or unsubstituted heteroaromatic, and wherein the group R1, R2 or R3 is a group of formula N(R)2 or N(COR)2, each of the R groups may be the same or different, or the two R groups, together with the nitrogen atom to which they are attached, m