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

Authors :: Spengler G
Ocsovszki I
Tönki ÁS
Saijo R
Watanabe G
Kawase M
Molnár J
Source :: Anticancer research [Anticancer Res] 2015 Nov; Vol. 35 (11), pp. 5915-9.
Publication Year :: 2015
Abstract: 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.<br /> (Copyright© 2015 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved.)

Subjects :: ATP Binding Cassette Transporter, Subfamily B antagonists & inhibitors
Animals
Drug Resistance, Multiple drug effects
Drug Resistance, Neoplasm drug effects
Flow Cytometry
Heterocyclic Compounds chemistry
Humans
Hydrocarbons, Fluorinated chemistry
Mice
Tumor Cells, Cultured
Vasodilator Agents pharmacology
Verapamil pharmacology
Cell Proliferation drug effects
Heterocyclic Compounds pharmacology
Hydrocarbons, Fluorinated pharmacology
Lymphoma, T-Cell drug therapy
Lymphoma, T-Cell pathology
Phosphorus chemistry

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