Bioorganic and medicinal chemistry letters (2020)
Update date:2022-08-11
Topics:
Abou Samra, Alma
Ariffin, Azhar
Awang, Khalijah
Bignon, Jérome
Daressy, Florian
Desrat, Sandy
Fourneau, Christophe
Gapil Tiamas, Shelly
Hoong Leong, Kok
Litaudon, Marc
Roussi, Fanny
Steinmetz, Vincent
A library of 26 novel carboxamides deriving from natural fislatifolic acid has been prepared. The synthetic strategy involved a bio-inspired Diels-Alder cycloaddition, followed by functionalisations of the carbonyl moiety. All the compounds were evaluated on Bcl-xL, Mcl-1 and Bcl-2 proteins. In this series of cyclohexenyl chalcone analogues, six compounds behaved as dual Bcl-xL/Mcl-1 inhibitors in micromolar range and one exhibited sub-micromolar affinities toward Mcl-1 and Bcl-2. The most potent compounds evaluated on A549 and MCF7 cancer cell lines showed moderate cytotoxicities.
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