Synthesis and antitumor activity of tropolone derivatives. 5.

Abstract

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.

• Authors: M Yamato, K Hashigaki, J Sakai, Y Takeuchi, S Tsukagoshi, T Tashiro, T Tsuruo
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 30 Issue 7 Pg. 1245-8 (Jul 1987) ISSN: 0022-2623 [Print] United States
• PMID: 3599030 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Cycloheptanes
• Tropolone

Topics

• Animals
• Antineoplastic Agents (chemical synthesis, pharmacology)
• Cycloheptanes (chemical synthesis)
• Mice
• Structure-Activity Relationship
• Tropolone (chemical synthesis, pharmacology)