Antitumor diarylsulfonylureas: novel agents with unfulfilled promise.

Diarylsulfonylureas represent a class of antitumor agent with significant therapeutic efficacy against rodent and human models of cancer. Despite the exciting preclinical activity of sulofenur, the prototypic agent, clinical activity was poor. Here we review the activity of sulofenur and a second generation diarylsulfonylurea, LY295501 N-[5-(2, 3-dihydrobenzofuryl) sulfonyl]-N'-(3,4-dichlorophenyl)urea, against colon tumor xenografts, and some of the cellular pharmacology of this class of antitumor agents.