Novel naphthalene-enoates: Design and anticancer activity through regulation cell autophagy - 04/04/19
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Graphical abstract |
Results of anticancer activity showed compound 4i could induce cancer cells apoptosis. Further experiments showed autophagy played an important role in the pro-apoptotic
Highlights |
• | New naphthalene derivatives were synthesized. |
• | Title compound could induce cancer cells apoptosis through autophagy. |
• | Preliminary mechanisms of anticancer were discovered. |
Abstract |
Eleven dihydroxy-2-(1-hydroxy-4-methylpent-3-enyl)naphthalene derivatives as anticancer agents through regulating cell autophagy were designed and synthesized. The anticancer activity results indicated that most compounds manifested obvious un-toxic effect on GES-1 and L-02 with IC50 from 0.58 to 1.41 mM. Among them, (S,Z)-1-(5,8-dihydroxy-1,4-dioxo-1,4-dihydronaphthalen-2-yl)-4-methylpent-3-enyl 4-(3,4-
dihydroisoquinolin-2(1 H)-yl)-4-oxobut-2-enoate (compound 4i) could induce cancer cells apoptosis. Further experiments showed that autophagy played an important role in the pro-apoptotic effect of this compound. Preliminary mechanism indicated that this compound could inhibit phosphoinositide 3-kinase/protein kinase B and the mammalian target of rapamycin (PI3K/AKT/mTOR) pathway by mediating apoptosis in an autophagy-dependent manner.
Le texte complet de cet article est disponible en PDF.Keywords : Synthesis, Naphthalene derivatives, Anticancer activity, Autophagy
Plan
Vol 113
Article 108747- mai 2019 Retour au numéro
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