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.
Export Options
About this article
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 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Metabolomics and the Diagnosis of Human Diseases -A Guide to the Markers and Pathophysiological Pathways Affected
Current Medicinal Chemistry Glucose Oncometabolism of Esophageal Cancer
Anti-Cancer Agents in Medicinal Chemistry Metabolomics-based Approach to Pharmacotherapy Personalization: Advantages and Limitations
Current Pharmacogenomics and Personalized Medicine Antagonists of IAP Proteins: Novel Anti-Tumor Agents
Current Medicinal Chemistry Application of MALDI/SELDI Mass Spectrometry to Cancer Biomarker Discovery and Validation
Current Proteomics Therapeutic Approach of Primary Bone Tumours by Bisphosphonates
Current Pharmaceutical Design Serine Protease Inhibitor Kazal Type 1 (SPINK1): Beyond the Trypsin Inhibitor
Current Enzyme Inhibition Angiogenesis Inhibitors: Implications for Combination with Conventional Therapies
Current Pharmaceutical Design Hsp70 Protein Complexes as Drug Targets
Current Pharmaceutical Design New Anti-Angiogenic Targeted Therapy in Advanced Renal Cell Carcinoma (RCC):Current Status and Future Prospects
Reviews on Recent Clinical Trials Bevacizumab and Angiogenesis Inhibitors in the Treatment of CNS Metastases: The Road less Travelled
Current Molecular Pharmacology MicroRNAs in Renal Cell Carcinoma
MicroRNA Targeted Therapies in the Treatment of Renal Cell Carcinoma
Current Medicinal Chemistry A Comprehensive Review on the Genetic Regulation of Cisplatin-induced Nephrotoxicity
Current Genomics Withdrawal Notice: The Recent Advancement in the Field of Super Paramagnetic Iron Oxide Nanoparticles (SPIONs) for Aiming Breast Cancer
Current Drug Metabolism Recent Advances in Structural Studies of the Carbonic Anhydrase Family: The Crystal Structure of Human CA IX and CA XIII
Current Pharmaceutical Design Mechanisms of Acquired Resistance to Tyrosine Kinase Inhibitors in Clear - Cell Renal Cell Carcinoma (ccRCC)
Current Signal Transduction Therapy Targeting Angiogenesis in Head and Neck Cancer
Current Cancer Drug Targets Targeted Radionuclide Therapy - An Overview
Current Radiopharmaceuticals Neuroprotective Effects of Non-Classical Estrogen-Like Signaling Activators: from Mechanism to Potential Implications
CNS & Neurological Disorders - Drug Targets