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

Abstract:

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

journal_name

Bioorg Med Chem Lett

authors

Sako M,Suzuki H,Yamamoto N,Hirota K

doi

10.1016/s0960-894x(99)00620-4

subject

Has Abstract

pub_date

1999-12-20 00:00:00

pages

3403-6

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960894X99006204

journal_volume

9

pub_type

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