Combretoxazolones: synthesis, cytotoxicity and antitumor activity.
Two series of combretoxazolones including 3,4-diaryloxazolones (6) and 4,5-diaryloxazolones (7) were synthesized and evaluated for cytotoxicity and antitumor activity. Both series showed strong cytotoxicities against a variety of tumor cell lines. Compound 6g exhibited a significant antitumor activity in BDF1 mice bearing B16 murine melanoma cells with inhibition rates of 67 and 61% at 100 and 30 mg/kg/day, respectively.
Nam
N H
NH
College of Pharmacy, Chungnam National University, Taejon 305-764, Republic of Korea.
Kim
Y
Y
You
Y J
YJ
Hong
D H
DH
Kim
H M
HM
Ahn
B Z
BZ
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D001671:Biochemistry / Q000379:methods; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D008545:Melanoma / Q000188:drug therapy; D051379:Mice; D008815:Mice, Inbred Strains; D010080:Oxazoles / Q000737:chemistry* / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D010080:Oxazoles