Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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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, Adam McCluskey.

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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Article Details

VOLUME: 6
ISSUE: 1
Year: 2009
Page: [1 - 7]
Pages: 7
DOI: 10.2174/157018009787158535