Isolation and Identification of the Novel Tubulin Polymerization Inhibitor Bifidenone.
Basic Information
ID: ALA4052612
Journal: J Nat Prod
Title: Isolation and Identification of the Novel Tubulin Polymerization Inhibitor Bifidenone.
Authors: Williams RB, Martin SM, Lawrence JA, Norman VL, O'Neil-Johnson M, Eldridge GR, Starks CM.
Abstract: The pursuit of structurally novel compounds has led to the isolation of a series of neolignans (2-6), for which the structures have been determined from microgram quantities using microcryoprobe NMR technology. Compounds 2-6 provided some unexpectedly clear structure-activity relationship data, with compound 2 demonstrating significantly more potency in the in vitro cytotoxicity assay than the other analogues. Further screening found that compound 2 induces apoptosis with activation of caspase 3/7. The NCI Compare algorithm suggested that compound 2 acts through the inhibition of tubulin/microtubule dynamics. Compound 2 was confirmed to be a tubulin polymerization inhibitor that binds directly to tubulin.
CiteXplore: 28335606
DOI: 10.1021/acs.jnatprod.6b00893
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