Pro-apoptotic carboxamide analogues of natural fislatifolic acid targeting Mcl-1 and Bcl-2

Shelly Gapil Tiamas, Florian Daressy, Alma Abou Samra, Jérome Bignon, Vincent Steinmetz, Marc Litaudon, Christophe Fourneau, Kok Hoong Leong, Azhar Ariffin, Khalijah Awang, Sandy Desrat, Fanny Roussi

    研究成果: Contribution to journalArticle査読

    1 被引用数 (Scopus)

    抄録

    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.

    本文言語英語
    論文番号127003
    ジャーナルBioorganic and Medicinal Chemistry Letters
    30
    7
    DOI
    出版ステータス出版済み - 4 1 2020

    All Science Journal Classification (ASJC) codes

    • Biochemistry
    • Molecular Medicine
    • Molecular Biology
    • Pharmaceutical Science
    • Drug Discovery
    • Clinical Biochemistry
    • Organic Chemistry

    フィンガープリント 「Pro-apoptotic carboxamide analogues of natural fislatifolic acid targeting Mcl-1 and Bcl-2」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。

    引用スタイル