Sunday, August 10, 2008
P105

Novel fungal natural products with bioactivity in a progesterone receptor reporter assay

Laurel R. Barbieri1, Ramunas Bigelis1, Li-Ping Chang1, Maya P. Singh1, Thomas Berrodin2, Matthew Yudt2, Leonard A. McDonald1, Daniel A. Arias1, and Deborah M. Roll1. (1) Natural Products Discovery Research, Wyeth Research, 401 North Middletown Road, Pearl River, NY 10965, (2) Women's Health & Musculoskeletal Biology, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426

Nonsteroidal progesterone receptor (PR) agonists have potential use as female contraceptives or in hormone therapy.  While screening our Natural Products microbial library for promising leads in a PR agonist assay, one crude fungal extract exhibited moderate activity and was prioritized for scaleup.  Using LCMS and bioassay-guided isolation, four novel nonsteroidal metabolites were purified from both solid and liquid culture fermentations.  The structure determination was based on analysis of UV, MS, and 2D NMR data.  One of the analogs was prioritized as an early lead in our screen for novel progesterone receptor agonists.  In this poster we describe the fermentation, isolation, structural analysis, and biological activity of the four new fungal analogs.

See more of Poster Session 1
See more of Posters

See more of The Annual Meeting and Exhibition 2008 (August 10 - 14, 2008)