Synthesis and antitumor activity of tropolone derivatives. 3

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Abstract
As part of a study on the antitumor activities of tropolone derivatives prepared from hinokitiol (1), which naturally occurs in the plants of Chamaecyparis species, effects of aromatic substituents of .alpha.,.alpha.-bis(7-hydroxy-5-isopropyltropon-2-yl)toluenes (4) on the activity were examined. Several of the compounds showed high potency in the P388 leukemia assay. 4-Hydroxy analogue 4d showed the most potent activity (T/C = 195%) at a 5 mg/kg dose. The introduction of large-size substituents, of which the steric influence prevents coplanarity of the substituted aromatic function, resulted in a remarkable decrease in the potency. X-ray structure analysis of highly potent 4-methoxy analogue 4b was undertaken.