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,...
0 downloads 0 Views

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

Downloaded via UNIV OF WINNIPEG on January 29, 2019 at 14:26:46 (UTC). See https://pubs.acs.org/sharingguidelines for options on how to legitimately share published articles.

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 (