Acid-catalyzed synthesis of 10-substituted triazolyl artemisinins and their growth inhibitory activity against various cancer cells
- Acid-catalyzed synthesis of 10-substituted triazolyl artemisinins and their growth inhibitory activity against various cancer cells
- 오상태; 신운섭; 함정엽; 이석준
- Artemisinin; Triazoyl artemisinin; Anticancer; Diastereomer; Regioisomer
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 20, NO 14, 4112-4115
- 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.
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