Acid-catalyzed synthesis of 10-substituted triazolyl artemisinins and their growth inhibitory activity against various cancer cells

Title
Acid-catalyzed synthesis of 10-substituted triazolyl artemisinins and their growth inhibitory activity against various cancer cells
Authors
오상태신운섭함정엽이석준
Keywords
Artemisinin; Triazoyl artemisinin; Anticancer; Diastereomer; Regioisomer
Issue Date
2010-07
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 20, NO 14, 4112-4115
Abstract
A diastereomeric and regioisomeric library of 10-substituted triazolyl artemisinin compounds (6a–6h, 7a–7h, and 8a–8h) with a potent growth inhibitory activities against various cancer cell lines was established. These compounds were synthesized by a reaction with dihydroartemisinin (2) and various substituted triazoles (5a–5h) in methylene chloride using a BF3Et2O catalyst. Most of the compounds exhibited a strong potency in the submicromolar range, and, in particular, 6f, 7f, and 8f, which have a pentylphenyltriazole moiety, proved to be promising candidates for preclinical trials.
URI
http://pubs.kist.re.kr/handle/201004/37615
ISSN
0960-894X
Appears in Collections:
KIST Publication > Article
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