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 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.
Morihira
K
K
Department of Chemistry, Tokyo Institute of Technology, Japan.
Nishimori
T
T
Kusama
H
H
Horiguchi
Y
Y
Kuwajima
I
I
Tsuruo
T
T
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
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D001952:Bridged-Ring Compounds; D043823:Taxoids; C080625:taxane; D014750:Vincristine; D014700:Verapamil