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

Title: 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

VOLUME: 6 ISSUE: 1

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

Affiliation:Chemistry, School of Environmental&Life Sciences, The University of Newcastle, Callaghan, NSW 2308, Australia.

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

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.

Cite this article as:

Benjamin Sauer, Jayne Gilbert, Jennette A. Sakoff and Adam McCluskey, “ 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”, Letters in Drug Design & Discovery (2009) 6: 1. https://doi.org/10.2174/157018009787158535

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