title: Synthesis of C-ring aromatic taxoids and evaluation of their multi-drug resistance reversing activity.
abstract: The C-aromatic taxoids were synthesized to develop effective inhibitors against 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.
authors.affiliation: Department of Chemistry, Tokyo Institute of Technology, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Morihira
authors.forename: T
authors.initials: T
authors.lastname: Nishimori
authors.forename: H
authors.initials: H
authors.lastname: Kusama
authors.forename: Y
authors.initials: Y
authors.lastname: Horiguchi
authors.forename: I
authors.initials: I
authors.lastname: Kuwajima
authors.forename: T
authors.initials: T
authors.lastname: Tsuruo
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors*; D001952:Bridged-Ring Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D018432:Drug Resistance, Multiple; D005260:Female; D006801:Humans; D013329:Structure-Activity Relationship; D043823:Taxoids; D014700:Verapamil / Q000494:pharmacology; D014750:Vincristine / Q000493:pharmacokinetics
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D001952:Bridged-Ring Compounds; D043823:Taxoids; C080625:taxane; D014750:Vincristine; D014700:Verapamil