Abstract
Traditional medicines have contributed greatly over the centuries to the discovery and development of new therapeutic agents and indoloquinoline alkaloids may represent a new class of drug leads. Cryptolepine (5-methyl-5H-indolo[ 3,2-b]quinoline), neocryptolepine (5-methyl-5H-indolo[2,3-b]quinoline), isocryptolepine (5-methyl-5H-indolo[3,2- c]quinoline, extracted from the African medicinal plant Cryptolepis sanguinolenta, and isoneocryptolepine (5-methyl-5H-indolo[ 2,3-c]quinoline), which has never been found in nature, are isomeric tetracyclic compounds of particular interest due to their broad spectrum of biological activities including antiparasitic, antifungal, antibacterial, cytotoxic, antiinflammatory and antihyperglycaemic. As a result, in the last 30 years hundreds of indoloquinoline analogues were synthesized and their biological activities evaluated. In this paper, we present an overview of the potential of indoloquinolines as scaffolds in drug discovery by reviewing the in vitro and in vivo biological activities of natural and synthetic analogues, as well as the proposed mechanisms of action and structure-activity relationships.
Keywords: Indoloquinolines, cryptolepine, isocryptolepine, neocryptolepine, isoneocryptolepine, structure-activity relationships (SAR), Cryptolepis sanguinolenta
Current Medicinal Chemistry
Title: Indoloquinolines as Scaffolds for Drug Discovery
Volume: 17 Issue: 22
Author(s): J. Lavrado, R. Moreira and A. Paulo
Affiliation:
Keywords: Indoloquinolines, cryptolepine, isocryptolepine, neocryptolepine, isoneocryptolepine, structure-activity relationships (SAR), Cryptolepis sanguinolenta
Abstract: Traditional medicines have contributed greatly over the centuries to the discovery and development of new therapeutic agents and indoloquinoline alkaloids may represent a new class of drug leads. Cryptolepine (5-methyl-5H-indolo[ 3,2-b]quinoline), neocryptolepine (5-methyl-5H-indolo[2,3-b]quinoline), isocryptolepine (5-methyl-5H-indolo[3,2- c]quinoline, extracted from the African medicinal plant Cryptolepis sanguinolenta, and isoneocryptolepine (5-methyl-5H-indolo[ 2,3-c]quinoline), which has never been found in nature, are isomeric tetracyclic compounds of particular interest due to their broad spectrum of biological activities including antiparasitic, antifungal, antibacterial, cytotoxic, antiinflammatory and antihyperglycaemic. As a result, in the last 30 years hundreds of indoloquinoline analogues were synthesized and their biological activities evaluated. In this paper, we present an overview of the potential of indoloquinolines as scaffolds in drug discovery by reviewing the in vitro and in vivo biological activities of natural and synthetic analogues, as well as the proposed mechanisms of action and structure-activity relationships.
Export Options
About this article
Cite this article as:
Lavrado J., Moreira R. and Paulo A., Indoloquinolines as Scaffolds for Drug Discovery, Current Medicinal Chemistry 2010; 17 (22) . https://dx.doi.org/10.2174/092986710791698521
DOI https://dx.doi.org/10.2174/092986710791698521 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- 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
- Announcements
Related Articles
-
Recent Progress in the Design and Discovery of RXR Modulators Targeting Alternate Binding Sites of the Receptor
Current Topics in Medicinal Chemistry Synthesis, Crystal Structure and Anti-HIV Activity of 2- Adamantyl/adamantylmethyl-5-aryl-1,3,4-oxadiazoles
Medicinal Chemistry Synthetic Thioamide, Benzimidazole, Quinolone and Derivatives with Carboxylic Acid and Ester Moieties: A Strategy in the Design of Antituberculosis Agents
Current Medicinal Chemistry Overview of Drug Therapy of COVID-19 with Safety and the Potential Clinical Benefits
Current Drug Therapy Integrating Virtual Screening and Combinatorial Chemistry for Accelerated Drug Discovery
Combinatorial Chemistry & High Throughput Screening Synthesis of Five-Membered Heterocycles Containing Nitrogen Heteroatom Under Ultrasonic Irradiation
Mini-Reviews in Organic Chemistry Cellular and Molecular Aspects of Managing Familial Hypercholesterolemia: Recent and Emerging Therapeutic Approaches
Endocrine, Metabolic & Immune Disorders - Drug Targets Antitumor Effects of Celastrol and Semi-Synthetic Derivatives
Mini-Reviews in Organic Chemistry Partial Order Theory Applied to QSPR-QSAR Studies
Combinatorial Chemistry & High Throughput Screening Oxocarbon Acids and their Derivatives in Biological and Medicinal Chemistry
Current Medicinal Chemistry Typical and Atypical Imaging Findings of Abdominal Teratomas
Current Medical Imaging Oxidative Stress and Antioxidant Potential of One Hundred Medicinal Plants
Current Topics in Medicinal Chemistry Open Source Software and Web Services for Designing Therapeutic Molecules
Current Topics in Medicinal Chemistry Chemical Connexin Impairment in the Developing Gonad Associated with Offspring Infertility
Current Medicinal Chemistry Brevifoliol and its Analogs: A New Class of Anti-tubercular Agents
Current Topics in Medicinal Chemistry Small Molecule Antagonists of the Chemokine Receptor CCR5
Current Topics in Medicinal Chemistry Novel Hybrid Molecules of Quinazoline Chalcone Derivatives: Synthesis and Study of in vitro Cytotoxic Activities
Letters in Drug Design & Discovery Coronavirus Pandemic: Role of Bats And Zoonotic Transmission in Humans
Coronaviruses BACE Inhibitors as Potential Drugs for the Treatment of Alzheimers Disease: Focus on Bioactivity
Recent Patents on CNS Drug Discovery (Discontinued) Recent Progress in the Development of Natural ent-Kaurane Diterpenoids with Anti-tumor Activity
Mini-Reviews in Medicinal Chemistry