Abstract
Previously, we designed and synthesized the 2,3,6,7-tetrahydro-1H-pyrrolo[1,2-a]indole-1,8(5H)-dione as a versatile structural platform to be functionalized to obtain potential DNA-interactive agents by intercalation and/or reversible enzyme inhibition. Herein, we report an alternative synthetic route for the preparation of this heterocyclic template as well as the synthesis of an its “two-armed” derivative. Also, a computational docking study to investigate the possible DNA-binding mode of well-known binders and title compound was performed.
Keywords: DNA binders, Docking, Intercalation, Two-armed derivatives, 2,3,6,7-Tetrahydro-1H-pyrrolo[1,2-a]indole- 1, 8(5H)-dione
Letters in Drug Design & Discovery
Title: DNA Binders: 1. Evaluation of DNA-Interactive Ability, Design, and Synthesis of Novel Intercalating Agents
Volume: 6 Issue: 1
Author(s): Mario Sechi, Marco Derudas, Roberto Dallocchio, Alessandro Dessì, Alessia Cosseddu and Giuseppe Paglietti
Affiliation:
Keywords: DNA binders, Docking, Intercalation, Two-armed derivatives, 2,3,6,7-Tetrahydro-1H-pyrrolo[1,2-a]indole- 1, 8(5H)-dione
Abstract: Previously, we designed and synthesized the 2,3,6,7-tetrahydro-1H-pyrrolo[1,2-a]indole-1,8(5H)-dione as a versatile structural platform to be functionalized to obtain potential DNA-interactive agents by intercalation and/or reversible enzyme inhibition. Herein, we report an alternative synthetic route for the preparation of this heterocyclic template as well as the synthesis of an its “two-armed” derivative. Also, a computational docking study to investigate the possible DNA-binding mode of well-known binders and title compound was performed.
Export Options
About this article
Cite this article as:
Sechi Mario, Derudas Marco, Dallocchio Roberto, Dessì Alessandro, Cosseddu Alessia and Paglietti Giuseppe, DNA Binders: 1. Evaluation of DNA-Interactive Ability, Design, and Synthesis of Novel Intercalating Agents, Letters in Drug Design & Discovery 2009; 6 (1) . https://dx.doi.org/10.2174/157018009787158472
DOI https://dx.doi.org/10.2174/157018009787158472 |
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
-
Proteomic Analysis of Intra- and Extracellular Proteins of <i>Aspergillus Niveus</i> During Submerged Bioprocess Culturing Under Different pH Conditions
Current Proteomics Recent Advancement in Topical Drug Delivery for Psoriasis: Clinical Pertinence and Potential Market
Current Drug Targets Phenylboronic Acid-polymers for Biomedical Applications
Current Medicinal Chemistry Classification of Sarcomas Using Bioinformatics and Molecular Profiling
Current Pharmaceutical Biotechnology Nanomaterials-based Polymerase Chain Reactions for DNA Detection
Current Organic Chemistry The Progress of Selective Fluorescent Chemosensors by Boronic Acid
Current Medicinal Chemistry Synthesis & Characterization of 2-(substituted-phenyl)acetohydrazide Analogs, 1,3,4-oxadiazoles, and 1,2,4-triazine Ring Systems: A Novel Class of Potential Analgesic and Anti-Inflammatory Agents
Letters in Drug Design & Discovery Carbonic Anhydrase Inhibitors
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Cinnamic Acid Derivatives as Anticancer Agents-A Review
Current Medicinal Chemistry Possible Targets of Herbals for Type 3 Diabetes: A Review
Current Traditional Medicine Magnetic Resonance-Based Metabolomics for Understanding Neurological Disorders: Current Status and Statistical Considerations
Current Metabolomics Sulfated Extract of <i>Abelmoschus Esculentus</i>: A Potential Cancer Chemo-preventive Agent
Current Pharmaceutical Biotechnology The Oxygen Therapy
Current Medicinal Chemistry Compounds Combining Aminoadamantane and Monoterpene Moieties: Cytotoxicity and Mutagenic Effects
Medicinal Chemistry Mass Spectrometric Imaging of the Nervous System
Current Pharmaceutical Design Fluorescent Carbon Dots and their Applications in Sensing of Small Organic Molecules
Current Analytical Chemistry Prediction of Mutations in H3N2 Hemagglutinins of Influenza A Virus from North America Based on Different Datasets
Protein & Peptide Letters Cyclodextrins and their Derivatives as Carrier Molecules in Drug and Gene Delivery Systems
Current Organic Chemistry The Study on the Fingerprint and Qualitative Analysis of Characteristic Volatile Constituens in Xihuang Pill by GC/GC-MS
Current Analytical Chemistry Synthesis of 2,5-Disubstituted-1,3,4-oxadiazole Analogs as Novel Anticancer and Antimicrobial Agents
Letters in Drug Design & Discovery