Variolin derivatives and their use as antitumor agents

Abstract

Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X, R, R, R, R, Rand Rare each independently selected from the group consisting of H, OH, OR', SH, SR′, SOR′, SOR′, NO, NH, NHR′, N(R′), NHCOR′, NHSOR′, CN, halogen, ═O, C(═O)H, C(═O)R′, COH, COR′, carboxyalkyl, C-Calkyl, C-Calkenyl, C-Calkynyl, 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, NO, NH, CN, halogen, ═O, C(═O)H, C(═O)CH, COH, COCH, C-Calkyl, C-Calkenyl, C-Calkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups Rand R, Rand R, Rand R, Rand R, or Rand Rmay be joined into a carbocyclic or heterocyclic ring system.