Synthetic studies on (E)-alkene peptide isosteres and thiophene-containing furanosteroids.

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Overview

Peptide isosteres are important tools for the understanding of peptide function and for the development of drugs. (E)-Alkene peptide isosteres are particularly useful due to their close geometric match of the amide bond structure. We developed a method for the generation of a small library of (E)-alkene peptide isosteres on solid support via cuprate mediated SN2' ring opening of allylic BUS-aziridines. We also studied the selectivity for the opening of these aziridines in the solution phase.;Halenaquinone is a marine natural product that was first isolated in 1983 from the Pacific sponge Xestosongia exigua. We realized the synthesis of a thiophene-containing analog, thio-halenaquinone. The key steps include an alkynyl ketone-benzocylcobutane Diels-Alder reaction to construct the naphthalene subunit, a Heck cyclization to form the quaternary carbon, and a ring closing metathesis to install the final ring. This compound showed an IC90 ∼5 muM against Pfnek-1 and an analog that had an IC90 ∼3 muM. Based on these results we designed and synthesized a simplified analog that showed an IC90 ∼4 muM. This compound was selected to move on to animal testing and the synthesis was optimized for the preparation of and 200 mg of the lead structure.
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Product Details

  • ISBN-13: 9781243565747
  • Publisher: BiblioLabsII
  • Publication date: 9/3/2011
  • Pages: 274
  • Product dimensions: 8.00 (w) x 10.00 (h) x 0.71 (d)

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