Sulfonimidamide Analogs of Oncolytic Sulfonylureas † ,1

A series of sulfonimidamide analogs of the oncolytic diarylsulfonylureas was synthesized and evaluated for (1) in vitro cytotoxicity against CEM cells, (2) in vivo antitumor activity against subaxillary implanted 6C3HED lymphosarcoma, and (3) metabolic breakdown to the o-sulfate of p-chloroaniline....

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Published inJournal of medicinal chemistry Vol. 40; no. 6; pp. 1018 - 1025
Main Authors Toth, John E, Grindey, Gerald B, Ehlhardt, William J, Ray, James E, Boder, George B, Bewley, Jesse R, Klingerman, Kim K, Gates, Susan B, Rinzel, Sharon M, Schultz, Richard M, Weir, Leonard C, Worzalla, John F
Format Journal Article
LanguageEnglish
Published American Chemical Society 14.03.1997
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Summary:A series of sulfonimidamide analogs of the oncolytic diarylsulfonylureas was synthesized and evaluated for (1) in vitro cytotoxicity against CEM cells, (2) in vivo antitumor activity against subaxillary implanted 6C3HED lymphosarcoma, and (3) metabolic breakdown to the o-sulfate of p-chloroaniline. The separated enantiomers of one sulfonimidamide analog displayed very different activities in the in vivo screening model. In general, several analogs demonstrated excellent growth inhibitory activity in the 6C3HED model when dosed orally or intraperitoneally. A correlative structure−activity relationship to the oncolytic sulfonylureas was not apparent.
Bibliography:Dedicated to the memory of Gerry Grindey.
Abstract published in Advance ACS Abstracts, February 15, 1997.
ark:/67375/TPS-1G4F63D7-D
istex:03A9418C104B35FA98BD0A8C445FFBF333C8E987
ISSN:0022-2623
1520-4804
DOI:10.1021/jm960673l