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ID: ALA3351486
Journal: Bioorg Med Chem Lett
Title: Pro-apoptotic meiogynin A derivatives that target Bcl-xL and Mcl-1.
Authors: Desrat S, Pujals A, Colas C, Dardenne J, Gény C, Favre L, Dumontet V, Iorga BI, Litaudon M, Raphaël M, Wiels J, Roussi F.
Abstract: The biological evaluation of a natural sesquiterpene dimer meiogynin A 1, is described as well as that of five non-natural analogues. Although active on a micromolar range on the inhibition of Bcl-xL/Bak and Mcl-1/Bid interaction, meiogynin A 1 is not cytotoxic on three cell lines that overexpress Bcl-xL and Mcl-1. Contrarily, one of its analogues 6 with an inverted configuration on the side chain and an aromatic moiety replacing the cyclohexane ring was active on both target proteins, cytotoxic on a micromolar range and was found to induce apoptosis through a classical pathway.
CiteXplore: 25266781