SULFONIMIDAMIDE ANALOGS OF ONCOLYTIC SULFONYLUREAS

A series of sulfonimidamide analogs of the oncolytic diarylsulfonylure as was synthesized and evaluated for (1) in vitro cytotoxicity against CEM cells, (2) in vivo antitumor activity against subaxillary implant ed 6C3HED lymphosarcoma, and (3) metabolic breakdown to the o-sulfate of p-chloroaniline, The separated enantiomers of one sulfonimidamide a nalog displayed very different activities in the in vivo screening mod el. In general, several analogs demonstrated excellent growth inhibito ry activity in the 6C3HED model when dosed orally or intraperitoneally . A correlative structure-activity relationship to the oncolytic sulfo nylureas was not apparent.