托酚酮衍生物的合成与抗肿瘤活性

Synthesis and antitumor activity of tropolone derivatives.

作者信息

Yamato M, Hashigaki K, Kokubu N, Tsuruo T, Tashiro T

出版信息

J Med Chem. 1984 Dec;27(12):1749-53. doi: 10.1021/jm00378a041.

Abstract

Treatment of tropolones with benzaldehyde diethyl acetals gave monotropolone (12) and bistropolone (13) derivatives at the benzylic position, whereas the related 1-ethoxyisochroman and the diethyl acetals of crotonaldehyde and cinnamaldehyde gave only the monotropolone derivatives (5, 10, or 11). The monotropolone derivatives (5, 10, 11, and 12) had poor potency against P388 leukemia in mice, but the bistropolone derivatives (13 and 14) showed significant potency and prolongation of life.

摘要

用苯甲醛二乙缩醛处理卓酚酮，在苄基位置得到单卓酚酮（12）和双卓酚酮（13）衍生物，而相关的1-乙氧基异苯并二氢吡喃以及巴豆醛和肉桂醛的二乙缩醛仅得到单卓酚酮衍生物（5、10或11）。单卓酚酮衍生物（5、10、11和12）对小鼠P388白血病的效力较差，但双卓酚酮衍生物（13和14）显示出显著的效力并延长了生存期。