Synthesis and antitumor activity of tropolone derivatives. 2

Article abstract of DOI:10.1021/jm00146a009

Structural requirement for antitumor activity of tropolone derivatives was explored. Isochroman derivatives and α,α-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 analogue were synthesized. Among them, three showed significant activity, but their potencies were considerably weaker than those of binary tropolone analogues.