2. Academic Validation
  3. Serendipity in discovery of proteasome inhibitors

Serendipity in discovery of proteasome inhibitors

  • Bioorg Med Chem Lett. 2012 May 15;22(10):3503-5. doi: 10.1016/j.bmcl.2012.03.086.
Derek Dunn 1,  Mohamed Iqbal,  Jean Husten,  Mark A Ator,  Sankar Chatterjee
Affiliations

Affiliation

  • 1 Cephalon Inc., 145 Brandywine Parkway, West Chester, PA 19380, United States.
PMID: 22503349 DOI: 10.1016/j.bmcl.2012.03.086
Abstract

Among its various catalytic activities, the 'chymotrypsin-like' activity of the Proteasome, a large multicatalytic proteinase complex has emerged as the focus of drug discovery efforts in Cancer therapy. Herein, a series of first generation (2S, 3R)-2-amino-3-hydroxybutyric acid derived Proteasome inhibitors that were discovered serendipitously en route to original goal of generating a series of sterically constrained oxazoline derivatives has been reported.

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