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Article Dans Une Revue Planta Medica Année : 2017

Synthetic modification of 9 alpha- and 9 beta-hydroxyparthenolide by Heck or acylation reactions and evaluation of cytotoxic activities

Résumé

Motivated by the widely reported anticancer activity of parthenolides and their derivatives, a series of new substituted parthenolides was efficiently synthesized. Structural modifications were performed at the C-9 and C-13 positions of 9 alpha- and 9 beta-hydroxyparthenolide, which were isolated from the aerial parts of Anvillea radiata. Twenty-one derivatives were synthesized and evaluated for their in vitro cytotoxic activity against HS-683, SK-MEL-28, A549, and MCF-7 human cancer cell lines using the MTT colorimetric assay. Among the derivatives, seven exhibited excellent activity compared to 5-fluorouracil and etoposide against the four cell lines tested, with IC50 values ranging from 1.1 to 9.4 mu M. [GRAPHICS] .
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hal-01604788 , version 1 (02-10-2017)

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Abderrahman El Bouakher, Badr Jismy, Hassan Allouchi, Eric Duverger, Latifa Barkaoui, et al.. Synthetic modification of 9 alpha- and 9 beta-hydroxyparthenolide by Heck or acylation reactions and evaluation of cytotoxic activities. Planta Medica, 2017, 83 (7), pp.661-671. ⟨10.1055/s-0042-119864⟩. ⟨hal-01604788⟩
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