Highly increased cellular accumulation of vincristine, a useful hydrophobic antitumor-drug, in multidrug-resistant solid cancer cells induced by a simply reduced taxinine

作者: Magoichi Sako , Hikokazu Suzuki , Noriyuki Yamamoto , Kosaku Hirota

DOI: 10.1016/S0960-894X(99)00620-4

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摘要: Regio- and/or chemo-selective reductions of taxinine (1a), a taxane diterpenoid readily obtainable from the needles Japanese yew (Taxus cuspidata), at 5-O-cinnamoyl and 4-exo-methylene moieties have been accomplished by catalytic hydrogenation over Pd/C or Rh/C to obtain 5-O-phenylpropionylated A (1b), 5-O-cyclohexylpropionylated (1c), 4,20-dihydrotaxinine (2a) in almost quantitative yields, respectively. Among them, taxoid 1b was found be highly effective increasing cellular accumulation vincristine multidrug-resistant human ovarian cancer cells compared with cases verapamil previously reported taxoids.

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