Synthesis and antitumor activity of tropolone derivatives. 2

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Abstract
Structural requirement for antitumor activity of tropolone derivatives was explored [using KB cells and mouse P388 leukemia]. Isochroman derivatives and .alpha.,.alpha.-disubstituted compounds were synthesized and their antitumor activities were tested. These nontroponoid derivatives were all inactive, implying that a tropolone ring is essential for the activity. Several compounds related to the monotropolone analog were synthesized. Some showed significant activity, but their potencies were considerably weaker than those of binary tropolone analogs.