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.