Synthesis and antitumor activity of tropolone derivatives. 5.
As part of a study on the structure-activity relationship of antitumor-active tropolone derivatives, a series of bistropone analogues, related to potently active bistropolone 1a, were synthesized and tested for their antitumor activity in in vitro (KB cell) and in vivo (leukemia P388 in mice) systems. The methoxytropones 3 and 5, hydroxytropothione 10, and (N-methylamino)tropones 12 and 13 were inactive in both systems. Methoxytropone 6 exhibited weak activity, whose potency was equal to that of monotropolone 2a.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D003508:Cycloheptanes / Q000138:chemical synthesis*; D051379:Mice; D013329:Structure-Activity Relationship; D014334:Tropolone / Q000138:chemical synthesis* / Q000494:pharmacology
D000970:Antineoplastic Agents; D003508:Cycloheptanes; D014334:Tropolone