New taxanes as highly efficient reversal agents for multidrug resistance in cancer cells.
New non-cytotoxic taxanes synthesized from 10-deacetylbaccatin III and special hydrophobic acylating agents show remarkable MDR reversal activity (< or = 99.8%) against drug-resistant human breast cancer cells when co-administered with paclitaxel or doxorubicin. This activity is ascribed to the highly efficient blocking of P-glycoprotein efflux by these new taxanes.
Ojima
I
I
Department of Chemistry, State University of New York at Stony Brook 11794-3400, USA.
Bounaud
P Y
PY
Takeuchi
C
C
Pera
P
P
Bernacki
R J
RJ
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D000818:Animals; D004305:Dose-Response Relationship, Drug; D018432:Drug Resistance, Multiple; D006801:Humans; D013329:Structure-Activity Relationship; D043823:Taxoids; D014315:Triterpenes / Q000737:chemistry* / Q000494:pharmacology; D014407:Tumor Cells, Cultured
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D043823:Taxoids; D014315:Triterpenes; C042213:10-deacetylbaccatine III