New analogues of the anticancer E7070: synthesis and pharmacology.

Cell cycle control in the G1 phase has attracted considerable attention in recent cancer research, because many of the important proteins involved in G1 progression or G1/S transition have been found to play a crucial role in proliferation, differentiation, transformation, and programmed cell death (apoptosis). E7070 is a novel antitumor sulfonamide, with a unique mode of action that affects G1 progression of the cell cycle. A series of compounds containing an N-[1-(3,4,5-trimethoxybenzyl)-1H-indol-5-yl]benzene sulfonamide, analogues of E7070, was synthesized and evaluated as potential antitumor agents. Cell cycle analysis with PC3 human prostate cancer cells revealed a cellular accumulation in the G1 phase.