Pironetin - ACS Publications - American Chemical Society

Jan 29, 2019 - cause cell cycle arrest at the G2/M phase, leading to apoptosis.4,7 Drugs that alter ..... 10.2, 5.5 Hz, 1H), 2.07 (td, J = 11.3, 10.3,...
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Brief Article Cite This: J. Med. Chem. XXXX, XXX, XXX−XXX

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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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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 (