Literature

Abstract

This study revealed that various alicyclic and acyclic compounds containing the 3-(3,4,5-trimethoxyphenyl)-2-propenoyl group displayed potent MDR reversal properties. In particular, a concentration of 4 microg/ml of 2,5-bis(3,4,5-trimethoxyphenylmethylene)cyclopentanone was 31 times more potent than verapamil as a MDR revertant. In general, they were selectively toxic to malignant rather than normal cells. Two representative compounds induced apoptosis in human HL-60 cells and markedly activated caspase-3.

DOI： 10.1016/j.bmc.2007.03.022

3-(3,4,5-Trimethoxyphenyl)-1-oxo-2-propene: A novel pharmacophore displaying potent multidrug resistance reversal and selective cytotoxicity

Bioorganic & Medicinal Chemistry 2007.0

Design, Synthesis, and in Vitro Activity of Catamphiphilic Reverters of Multidrug Resistance: Discovery of a Selective, Highly Efficacious Chemosensitizer with Potency in the Nanomolar Range

Journal of Medicinal Chemistry 1999.0

1-[4-(2-Aminoethoxy)phenylcarbonyl]-3,5-bis-(benzylidene)-4-oxopiperidines: A novel series of highly potent revertants of P-glycoprotein associated multidrug resistance

Bioorganic & Medicinal Chemistry Letters 2008.0

1-[3-(2-Hydroxyethylsulfanyl)propanoyl]-3,5-bis(benzylidene)-4-piperidones: A novel cluster of P-glycoprotein dependent multidrug resistance modulators

Bioorganic & Medicinal Chemistry Letters 2016.0

1-(3,4,5-Trimethoxyphenyl)ethane-1,2-diyl esters, a novel compound class with potent chemoreversal activity

Bioorganic & Medicinal Chemistry Letters 2012.0

2-(3-Aryl-2-propenoyl)-3-methylquinoxaline-1,4-dioxides: A novel cluster of tumor-specific cytotoxins which reverse multidrug resistance