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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis of 4-substituted-3-hydroxy-5-oxo-10-oxa-4-azatricyclo[5.2.1]dec- 3-yl Acetic Acid Ethyl Esters as Norcantharidin Analogues

Author(s): Benjamin Sauer, Jayne Gilbert, Jennette A. Sakoff and Adam McCluskey

Volume 6, Issue 1, 2009

Page: [1 - 7] Pages: 7

DOI: 10.2174/157018009787158535

Price: $65

Abstract

A novel library of eighteen 4-substituted-3-hydroxy-5-oxo-10-oxa-4-azatricyclo[5.2.1]dec-3-yl acetic acid ethyl esters was generated in high yield in two steps from norcantharidin, a known protein phosphatase 1 and 2A inhibitor that displays good anticancer activity. Interestingly these analogues are bereft of anticancer and protein phosphatase activity, but possess the attributes needed for medicinal agents and could be used as scaffolds in other targets.

Keywords: Norcantharidin, Wittig reaction, Protein phosphatase 1 and 2A, Anticancer, Drug design scaffold

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