Pro-apoptotic meiogynin A derivatives that target Bcl-xL and Mcl-1. - Archive ouverte HAL
Article Dans Une Revue Bioorganic and Medicinal Chemistry Letters Année : 2014

Pro-apoptotic meiogynin A derivatives that target Bcl-xL and Mcl-1.

Résumé

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.

Domaines

Chimie organique
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Dates et versions

hal-01077156 , version 1 (07-03-2021)

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Sandy Desrat, Anaïs Pujals, Claire Colas, Jérémy Dardenne, Loëtitia Favre, et al.. Pro-apoptotic meiogynin A derivatives that target Bcl-xL and Mcl-1.. Bioorganic and Medicinal Chemistry Letters, 2014, 24 (21), pp.5086-5088. ⟨10.1016/j.bmcl.2014.09.004⟩. ⟨hal-01077156⟩
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