Synthesis and antitumor activity of tropolone derivatives. 1
作者:Masatoshi Yamato、Kuniko Hashigaki、Nobuhiko Kokubu、Takashi Tsuruo、Tazuko Tashiro
DOI:10.1021/jm00378a041
日期:1984.12
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
用苯甲醛二乙基乙缩醛处理对苯二酚在苄基位置得到单托酚酮(12)和双酮醚酮(13)衍生物,而相关的1-乙氧基异苯并二氢吡喃和巴豆醛和肉桂醛的二乙缩醛仅产生单托酚酮衍生物(5、10或11)。 。在小鼠中,单马酚酮衍生物(5、10、11和12)对P388白血病的效力较弱,而双马酚酮衍生物(13和14)则具有显着的效力和寿命延长。