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(5Z)-7-Oxozeaenol: A Novel and Potent Resorcylic Acid Lactone Kinase Inhibitor With a Cis-Enone Michael Acceptor

(5Z)-7-Oxozeaenol: A Novel and Potent Resorcylic Acid Lactone Kinase Inhibitor With a Cis-Enone Michael Acceptor

George A Ellestad

Chirality. 2019 Feb;31(2):110-117.

PMID: 30565749

Abstract:

In this review, evidence is presented from a number of research groups over the past two decades that show that (5Z)-7-oxozeaenol, an initially biologically uninteresting fungal metabolite, is a remarkably selective and potent kinase inhibitor with important antiproliferative and anti-inflammatory properties. Taken together, this research shows (5Z)-7-oxozeaenol to be a surprisingly selective and competitive ATP binder in which the aromatic ring of the resorcylic lactone mimics the adenine ring of ATP; that it binds covalently to a conserved cysteine at a metabolically unstable cis-enone Michael acceptor; the conformational importance of the macrocycle, which depends on the absolute stereochemistry and hydrogen bonding properties of the 8,9-diol; and the success of medicinal chemistry in stabilizing the cis-enone.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP253863193	5Z-7-Oxozeaenol		253863-19-3	Price

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