Structure−Activity Relationship of Polyisoprenyl Benzophenones from Garcinia pyrifera on the Tubulin/Microtubule System

Microtubule disassembly inhibitory properties have been established for the known polyisoprenylated benzophenones xanthochymol (1a) and guttiferone E (1b). The compounds were isolated from the fruits of Garcinia pyrifera collected in Malaysia. A structure−activity relationship study, including natur...

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Bibliographic Details
Published in:Journal of natural products (Washington, D.C.) D.C.), 2000-08, Vol.63 (8), p.1070-1076
Main Authors: Roux, Delphine, Hadi, Hamid A, Thoret, Sylviane, Guénard, Daniel, Thoison, Odile, Païs, Mary, Sévenet, Thierry
Format: Article
Language:English
Subjects:
Benzophenones - chemistry
Benzophenones - pharmacology
Biological and medical sciences
Butadienes - chemistry
Butadienes - pharmacology
Chromatography, Gel
Chromatography, High Pressure Liquid
Fruit - chemistry
Gas Chromatography-Mass Spectrometry
General pharmacology
Hemiterpenes
Humans
KB Cells - drug effects
Magnetic Resonance Spectroscopy
Malaysia
Medical sciences
Microtubules - drug effects
Optical Rotation
Pentanes
Pharmacognosy. Homeopathy. Health food
Pharmacology. Drug treatments
Plants, Medicinal - chemistry
Rosales - chemistry
Spectrophotometry, Infrared
Spectrophotometry, Ultraviolet
Structure-Activity Relationship
Tubulin - analysis
Tubulin - biosynthesis
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Summary:Microtubule disassembly inhibitory properties have been established for the known polyisoprenylated benzophenones xanthochymol (1a) and guttiferone E (1b). The compounds were isolated from the fruits of Garcinia pyrifera collected in Malaysia. A structure−activity relationship study, including natural and semisynthetic derivatives, delineated some structural features necessary for the interaction with tubulin within this compound class.
ISSN:0163-3864
1520-6025
DOI:10.1021/np0000872