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

Journal Name: Letters in Drug Design & Discovery

Volume 6 , Issue 1 , 2009

Become EABM
Become Reviewer

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

promotion: free to download

Rights & PermissionsPrintExport Cite as

Article Details

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

Article Metrics

PDF: 18