Brief Article Cite This: J. Med. Chem. XXXX, XXX, XXX−XXX
Identiﬁcation of the Metabolic Proﬁle of the α‑Tubulin-Binding Natural Product (−)−Pironetin Sara K. Coulup, David S. Huang, Henry L. Wong, and Gunda I. Georg* Department of Medicinal Chemistry and Institute for Therapeutics Discovery and Development, University of Minnesota, 717 Delaware Street SE, Minneapolis, Minnesota 55414, United States
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S Supporting Information *
ABSTRACT: Pironetin, the only crystallographically conﬁrmed natural product to target α-tubulin, displays potent cytotoxic activity against sensitive and resistant A2780 ovarian cancer cell lines but is only marginally active in vivo. We now report that pironetin has a short half-life (