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
Letters in Drug Design & Discovery
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:
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.
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Cite this article as:
Sauer Benjamin, Gilbert Jayne, Sakoff A. Jennette and McCluskey Adam, 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://dx.doi.org/10.2174/157018009787158535
DOI https://dx.doi.org/10.2174/157018009787158535 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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