Fluorinated beta-Diketo Phosphorus Ylides Are Novel Inhibitors of the ABCB1 Efflux Pump of Cancer Cells

Efflux pump inhibitors are attractive compounds that reverse multidrug resistance (MDR) in cancer cells. In the present study, 10 phosphorus ylides (P-ylides) were compared based on their MDR-reverting activity in human ATP-binding cassette sub-family B member 1 (ABCB1; P-glycoprotein) gene-transfec...

Teljes leírás

Elmentve itt :
Bibliográfiai részletek
Szerzők: Spengler Gabriella
Ocsovszki Imre
Szabó Tönki Ádám
Saijo Ryosuke
Watanabe Genki
Kawase Masami
Molnár József
Dokumentumtípus: Cikk
Megjelent: 2015
Sorozat:ANTICANCER RESEARCH 35 No. 11
mtmt:2962208
Online Access:http://publicatio.bibl.u-szeged.hu/10439
Leíró adatok
Tartalmi kivonat:Efflux pump inhibitors are attractive compounds that reverse multidrug resistance (MDR) in cancer cells. In the present study, 10 phosphorus ylides (P-ylides) were compared based on their MDR-reverting activity in human ATP-binding cassette sub-family B member 1 (ABCB1; P-glycoprotein) gene-transfected L5178Y mouse T-lymphoma cells. Among them, three P-ylides, Ph3P=C(COCF3)COPh, Ph3P=C(COC2F5)COPh and Ph3P=C(COC3F7)COPh were identified as selectively modulating the ABCB1 pump. These compounds, with low cytotoxicity against mouse T-lymphoma cells, exhibited more potency than the positive control ABCB1 inhibitor verapamil.
Terjedelem/Fizikai jellemzők:5915-5919
ISSN:0250-7005