Sulfonimidamide Analogs of Oncolytic Sulfonylureas,1

Autor:	Richard M. Schultz, William J. Ehlhardt, John F. Worzalla, Jesse R. Bewley, John E. Toth, Kim K. Klingerman, James Edward Ray, George B. Boder, Gerald B. Grindey, Sharon M. Rinzel, Susan B. Gates, Leonard C. Weir
Rok vydání:	1997
Předmět:	Pharmacokinetics Biochemistry Chemistry Oral administration In vivo Ratón Drug Discovery Molecular Medicine Metabolism Pharmacology Chemical synthesis In vitro Oncolytic virus
Zdroj:	Journal of Medicinal Chemistry. 40:1018-1025
ISSN:	1520-4804 0022-2623
DOI:	10.1021/jm960673l
Popis:	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.
Databáze:	OpenAIRE
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