Structure-activity studies on 2-aryl-4H-3, 1 -benzoxazin-4-ones

Eight benzoxazin-4-ones related In structure to NSC 341964 (1) have been tested for cytotoxlclty In two different cell systems. Two of the benzoxazln-4-ones (3 and 10) showed good cytotoxlclty (ID50 =9.9 and 8.9 µM) In P388 cells. The nltrobenzoxazln-4-one (10) caused a significant alteration in cel...

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Veröffentlicht in:	Anti-cancer drugs 1994-10, Vol.5 (5), p.533-538
Hauptverfasser:	Hadfleld, John A, Pavlidis, Vasilios H, McGown, Alan T, Whltworth, Caroline, Perry, Philip J, Fox, Brian W
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic Agents - pharmacology DNA, Neoplasm - metabolism Drug Screening Assays, Antitumor Female Humans KB Cells Leukemia P388 - drug therapy Magnetic Resonance Spectroscopy Mice Mice, Inbred DBA Models, Molecular Oxazines - pharmacology Pancreatic Elastase - antagonists & inhibitors Structure-Activity Relationship Swine Tetrazolium Salts Thiazoles Tumor Cells, Cultured
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Zusammenfassung:	Eight benzoxazin-4-ones related In structure to NSC 341964 (1) have been tested for cytotoxlclty In two different cell systems. Two of the benzoxazln-4-ones (3 and 10) showed good cytotoxlclty (ID50 =9.9 and 8.9 µM) In P388 cells. The nltrobenzoxazln-4-one (10) caused a significant alteration in cell cycle distribution when administered to P388 cells and was an inhibitor of porcine pancreatic elastase. Structure-activity relationships are discussed.
ISSN:	0959-4973 1473-5741
DOI:	10.1097/00001813-199410000-00004