Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 65, Issue -, Pages 158-167Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.04.057
Keywords
Pharmacophore similarity; Vinca alkaloid; Antimitotic agent; Anticancer
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Funding
- National Natural Science Foundation of China [81172982, 30901847, 30901848]
- Guangdong Provincial Project of Science and Technology [2010A030100006]
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Thorough simplification of vinca alkaloids based on pharmacophore similarity has been conducted. A concise process for the syntheses of target compounds was successfully developed with yields from poor to excellent (19-98%). Cell growth inhibitory activities of these synthesized compounds were evaluated in five cancer cell lines including MCF-7, MDA-MB-231, HepG2, HepG2/ADM and K562. Almost all compounds exhibited moderate antitumor activity with optimal IC50 value of 0.89 +/- 0.07 mu M in MCF-7 cells. Investigation of structure-activity relationship (SAR) indicates that electron-withdraw substituents on the ring contribute to the enhancement of the antitumor activities. The simplified vinca alkaloids are confirmed as antimitotic agents, which inhibit the polymerization of tubulin just like vinblastine. (C) 2013 Elsevier Masson SAS. All rights reserved.
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