Developing neolignans as proangiogenic agents: Stereoselective total syntheses and preliminary biological evaluations of the four guaiacylglycerol 8-O-4'-coniferyl ethers

Joshua N. Buckler, Martin G. Banwell*, Farzaneh Kordbacheh, Christopher R. Parish, Fernando S. Santiago, Levon M. Khachigian

*Corresponding author for this work

    Research output: Contribution to journalArticlepeer-review

    7 Citations (Scopus)

    Abstract

    Stereoselective total syntheses of the four stereoisomeric forms of guaiacylglycerol 8-O-4'-coniferyl ether, viz., compounds 1, ent-1, 2, and ent-2, have been established. The key step involves an Evans/Seebach auxiliarycontrolled and syn-selective aldol process followed, in the reaction sequences leading to the anti-compounds, by a Mitsunobu reaction involving a benzylic alcohol residue. The proangiogenic properties of the synthetic materials were evaluated in a human microvascular endothelial cell tubule formation assay, thus revealing that they are all active, with the 8S-configured compounds 1 and 2 being the most potent.

    Original languageEnglish
    Pages (from-to)7375-7388
    Number of pages14
    JournalACS Omega
    Volume2
    Issue number10
    DOIs
    Publication statusPublished - 31 Oct 2017

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