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 cytotoxicity in two different cell systems. Two of the benzoxazin-4-ones (3 and 10) showed good cytotoxicity (ID50 = 9.9 and 8.9 microM) in P388 cells. The nitrobenzoxazin-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.
CRC Department of Experimental Chemotherapy, Paterson Institute for Cancer Research, Christie Hospital, Manchester, UK.
J A
JA
Hadfield
V H
VH
Pavlidis
A T
AT
McGown
C
C
Whitworth
P J
PJ
Perry
B W
BW
Fox
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D004273:DNA, Neoplasm / Q000378:metabolism; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D007624:KB Cells; D007941:Leukemia P388 / Q000188:drug therapy; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D008811:Mice, Inbred DBA; D008958:Models, Molecular; D010078:Oxazines / Q000494:pharmacology*; D010196:Pancreatic Elastase / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship; D013552:Swine; D013778:Tetrazolium Salts; D013844:Thiazoles; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D004273:DNA, Neoplasm; D010078:Oxazines; D013778:Tetrazolium Salts; D013844:Thiazoles; D010196:Pancreatic Elastase; C022616:thiazolyl blue