Cytotoxic Activity of Some Natural and Synthetic Guaianolides

Several natural guaianolides and synthetic derivatives of repin (1) were tested and found to be active against tumor cell replication. Repin (1) and both mono- and di-halohydrin analogues (2, 7−9, 11, 12) showed significant antitumor potency. A more effective compound (17) was obtained by esterifica...

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Bibliographic Details
Published in:Journal of natural products (Washington, D.C.) D.C.), 2005-07, Vol.68 (7), p.1042-1046
Main Authors: Bruno, Maurizio, Rosselli, Sergio, Maggio, Antonella, Raccuglia, Rosa Angela, Bastow, Kenneth F, Lee, Kuo-Hsiung
Format: Article
Language:English
Subjects:
anticarcinogenic activity
Antineoplastic agents
Antineoplastic Agents, Phytogenic - chemical synthesis
Antineoplastic Agents, Phytogenic - isolation & purification
Antineoplastic Agents, Phytogenic - pharmacology
babylin
Biological and medical sciences
cebellin
Centaurea
Centaurea babylonica
chemical structure
chlorohyssopifolin
cultured cells
cytotoxicity
Drug Screening Assays, Antitumor
General aspects
guaianolides
human health
Humans
janerin
Medical sciences
medicinal plants
Molecular Structure
Paclitaxel - chemical synthesis
Paclitaxel - chemistry
Paclitaxel - pharmacology
Pharmacology. Drug treatments
phytochemicals
plant biochemistry
repin
Sesquiterpenes - chemical synthesis
Sesquiterpenes - isolation & purification
Sesquiterpenes - pharmacology
sesquiterpenoid lactones
sesquiterpenoids
spectral analysis
Structure-Activity Relationship
Tumor Cells, Cultured
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Description
Summary:Several natural guaianolides and synthetic derivatives of repin (1) were tested and found to be active against tumor cell replication. Repin (1) and both mono- and di-halohydrin analogues (2, 7−9, 11, 12) showed significant antitumor potency. A more effective compound (17) was obtained by esterificating repin with the paclitaxel side chain.
ISSN:0163-3864
1520-6025
DOI:10.1021/np0500575