Synthesis of c-ring aromatic taxoids and evaluation of their multi-drug resistance reversing activity

The C-aromatic taxoids were synthesized to develop effective inhibitors againts drug efflux mediated by p-glycoproteins. Among those tested using multi-drug resistant tumor cells (2780AD), the benzoate 11 exhibited significant activity as potent as verapamil, a well-established MDR reversing agent.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1998-11, Vol.8 (21), p.2973-2976
Main Authors: Morihira, Koichiro, Nishimori, Toshiyuki, Kusama, Hiroyuki, Horiguchi, Yoshiaki, Kuwajima, Isao, Tsuruo, Takashi
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastics
Antitumor compds
ATP-Binding Cassette, Sub-Family B, Member 1 - antagonists & inhibitors
Biological and medical sciences
Bridged-Ring Compounds - chemical synthesis
Bridged-Ring Compounds - pharmacology
Drug Resistance, Multiple
Female
General aspects
Humans
Medical sciences
Pharmacology. Drug treatments
Structure-Activity Relationship
Taxoids
Terpenes and terpenoids
Verapamil - pharmacology
Vincristine - pharmacokinetics
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Description
Summary:The C-aromatic taxoids were synthesized to develop effective inhibitors againts drug efflux mediated by p-glycoproteins. Among those tested using multi-drug resistant tumor cells (2780AD), the benzoate 11 exhibited significant activity as potent as verapamil, a well-established MDR reversing agent.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(98)00539-3