title: 3-(3,4,5-Trimethoxyphenyl)-1-oxo-2-propene: a novel pharmacophore displaying potent multidrug resistance reversal and selective cytotoxicity.
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.
authors: College of Pharmacy and Nutrition, University of Saskatchewan, 110 Science Place, Saskatoon, Canada SK S7N 5C9.
authors: Umashankar
authors: U
authors: Das
authors: Masami
authors: M
authors: Kawase
authors: Hiroshi
authors: H
authors: Sakagami
authors: Atsushi
authors: A
authors: Ideo
authors: Jun
authors: J
authors: Shimada
authors: Joseph
authors: J
authors: Molnár
authors: Zoltán
authors: Z
authors: Baráth
authors: Zsuzsanna
authors: Z
authors: Bata
authors: Jonathan R
authors: JR
authors: Dimmock
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D020169:Caspases / Q000378:metabolism; D045744:Cell Line, Tumor; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D019008:Drug Resistance, Neoplasm / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D004789:Enzyme Activation / Q000187:drug effects; D018922:HL-60 Cells; D006801:Humans; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D011407:Propane / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D013050:Spectrometry, Fluorescence
chemical_list: C520655:3-(3,4,5-trimethoxyphenyl)-1-oxo-2-propene; D000970:Antineoplastic Agents; D007202:Indicators and Reagents; D020169:Caspases; D011407:Propane