Abstract
9H-carbazole is an aromatic molecule that is tricyclic in nature, with two benzene rings fused onto a 5-membered pyrrole ring. Obtained from natural sources or by synthetic routes, this scaffold has gained much interest due to its wide range of biological activity upon modifications, including antibacterial, antimalarial, anticancer, and anti-Alzheimer properties. This review reports a survey of the literature on carbazole-containing molecules and their medicinal activities from 2010 through 2015. In particular, we focus on their in vitro and in vivo activities and summarize structure-activity relationships (SAR), mechanisms of action, and/or cytotoxicity/selectivity findings when available to provide future guidance for the development of clinically useful agents from this template.
Keywords: Biological activity, Carbazole, Natural product, SAR, Scaffold, Small molecule
Current Topics in Medicinal Chemistry
Title:Carbazole Scaffold in Medicinal Chemistry and Natural Products: A Review from 2010-2015
Volume: 16 Issue: 11
Author(s): Lissa S. Tsutsumi, Daniela Gündisch and Dianqing Sun
Affiliation:
Keywords: Biological activity, Carbazole, Natural product, SAR, Scaffold, Small molecule
Abstract: 9H-carbazole is an aromatic molecule that is tricyclic in nature, with two benzene rings fused onto a 5-membered pyrrole ring. Obtained from natural sources or by synthetic routes, this scaffold has gained much interest due to its wide range of biological activity upon modifications, including antibacterial, antimalarial, anticancer, and anti-Alzheimer properties. This review reports a survey of the literature on carbazole-containing molecules and their medicinal activities from 2010 through 2015. In particular, we focus on their in vitro and in vivo activities and summarize structure-activity relationships (SAR), mechanisms of action, and/or cytotoxicity/selectivity findings when available to provide future guidance for the development of clinically useful agents from this template.
Export Options
About this article
Cite this article as:
Tsutsumi S. Lissa, Gündisch Daniela and Sun Dianqing, Carbazole Scaffold in Medicinal Chemistry and Natural Products: A Review from 2010-2015, Current Topics in Medicinal Chemistry 2016; 16 (11) . https://dx.doi.org/10.2174/1568026615666150915112647
DOI https://dx.doi.org/10.2174/1568026615666150915112647 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
-
Preface: Unraveling Natures Secrets, from Neurons and Memory to Brain Disorders: Exploring the New Frontier of Alzheimers Disease
Current Alzheimer Research From Disorder to Mis-Order: Structural Aspects of Pathogenic Oligomerization in Conformational Diseases
Protein & Peptide Letters Triptolide Rescues Spatial Memory Deficits and Amyloid-β Aggregation Accompanied by Inhibition of Inflammatory Responses and MAPKs Activity in APP/PS1 Transgenic Mice
Current Alzheimer Research Diffusion Tensor Imaging to Determine Effects of Antidementive Treatment on Cerebral Structural Connectivity in Alzheimer’s Disease
Current Pharmaceutical Design Kefir: A Synbiotic with Approved Anticarcinogenic Properties
Current Bioactive Compounds Role of Cannabinoids and Endocannabinoids in Cerebral Ischemia
Current Pharmaceutical Design The Effects of Dehydroepiandrosterone (DHEA) in the Treatment of Depression and Depressive Symptoms in Other Psychiatric and Medical Illnesses: A Systematic Review
Current Drug Targets Diabetes and Nutritional Screening in Post-Bariatric Patients
Current Diabetes Reviews Pharmacological Influencing of The Cholinergic Anti-inflammatory Pathway in Infectious Diseases and Inflammatory Pathologies
Mini-Reviews in Medicinal Chemistry Evolutionary Considerations on the Emerging Subculture of the E-psychonauts and the Novel Psychoactive Substances: A Comeback to the Shamanism?
Current Neuropharmacology Role of Renin-Angiotensin System in Inflammation, Immunity and Aging
Current Pharmaceutical Design Human Imprinting Anomalies in Fetal and Childhood Growth Disorders: Clinical Implications and Molecular Mechanisms
Current Pharmaceutical Design The Impact of Depressive Symptoms on the Quality of Life of Patients with Type 2 Diabetes in Jazan Region, KSA
Current Diabetes Reviews Recent Innovations in Off-Road Intelligent Vehicles: In-Field Automatic Navigation
Recent Patents on Mechanical Engineering A synopsis on the linkage between age-related dementias and vascular disorders
CNS & Neurological Disorders - Drug Targets Innate Inflammatory Responses in Stroke: Mechanisms and Potential Therapeutic Targets
Current Medicinal Chemistry Inhibitors of NAD+ Dependent Histone Deacetylases (Sirtuins)
Current Pharmaceutical Design α/βHydrolase Fold: An Update
Protein & Peptide Letters Genetic Features of MAPT, GRN, C9orf72 and CHCHD10 Gene Mutations in Chinese Patients with Frontotemporal Dementia
Current Alzheimer Research The Antiproliferative and Pro-apoptotic Effects of Methoxyamine on Pediatric Medulloblastoma Cell Lines Exposed to Ionizing Radiation and Chemotherapy
Central Nervous System Agents in Medicinal Chemistry