Abstract
Alkaloid molecules can act, depending on a type of amine functionality present in alkalods, as either hydrogenacceptor or hydrogen-donor for hydrogen bonding that is critically important for the interaction (binding) between targets (enzymes, proteins and receptors) and drugs (ligands). Because of this unique property, alkaloid scaffolds are therefore present in several drugs and lead compounds. This review highlights alkaloid scaffolds in drugs, particularly those recently approved in 2012; it also covers the scaffolds in leads and drug candidates which are in clinical trials and preclinical pipeline. The review focuses on three therapeutic areas including treatments of cancer, tuberculosis, and tobacco cessation. Alkaloid scaffolds in drugs and leads are inspired by those of naturally occurring alkaloids, and these scaffolds include pyridine, piperidine, quinoline, quinolinone, quinazoline, isoquinoline, indole, indolinone, isoindole, isoxazole, imidazole, indazole, thiazole, pyrazole, oxazolidinone, oxadiazole, and benzazepine. In addition to medicinal chemistry aspects, natural products possessing an individual alkaloid scaffold, as well as the mechanism of action of drugs and leads, are also discussed in this review.
Keywords: Alkaloids, natural products, drugs, lead compounds, cancer, anticancer drugs, cytotoxic activity, antitubercular activity, antimycobacterial activity, tuberculosis, smoking cessation.
Current Topics in Medicinal Chemistry
Title:Alkaloids as Important Scaffolds in Therapeutic Drugs for the Treatments of Cancer, Tuberculosis, and Smoking Cessation
Volume: 14 Issue: 2
Author(s): Prasat Kittakoop, Chulabhorn Mahidol and Somsak Ruchirawat
Affiliation:
Keywords: Alkaloids, natural products, drugs, lead compounds, cancer, anticancer drugs, cytotoxic activity, antitubercular activity, antimycobacterial activity, tuberculosis, smoking cessation.
Abstract: Alkaloid molecules can act, depending on a type of amine functionality present in alkalods, as either hydrogenacceptor or hydrogen-donor for hydrogen bonding that is critically important for the interaction (binding) between targets (enzymes, proteins and receptors) and drugs (ligands). Because of this unique property, alkaloid scaffolds are therefore present in several drugs and lead compounds. This review highlights alkaloid scaffolds in drugs, particularly those recently approved in 2012; it also covers the scaffolds in leads and drug candidates which are in clinical trials and preclinical pipeline. The review focuses on three therapeutic areas including treatments of cancer, tuberculosis, and tobacco cessation. Alkaloid scaffolds in drugs and leads are inspired by those of naturally occurring alkaloids, and these scaffolds include pyridine, piperidine, quinoline, quinolinone, quinazoline, isoquinoline, indole, indolinone, isoindole, isoxazole, imidazole, indazole, thiazole, pyrazole, oxazolidinone, oxadiazole, and benzazepine. In addition to medicinal chemistry aspects, natural products possessing an individual alkaloid scaffold, as well as the mechanism of action of drugs and leads, are also discussed in this review.
Export Options
About this article
Cite this article as:
Kittakoop Prasat, Mahidol Chulabhorn and Ruchirawat Somsak, Alkaloids as Important Scaffolds in Therapeutic Drugs for the Treatments of Cancer, Tuberculosis, and Smoking Cessation, Current Topics in Medicinal Chemistry 2014; 14 (2) . https://dx.doi.org/10.2174/1568026613666131216105049
DOI https://dx.doi.org/10.2174/1568026613666131216105049 |
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
-
Antimicrobial and Antifungal Properties of Leaves to Root Extracts and Saponin Fractions of <i>Chlorophytum borivilianum</i>
Current Bioactive Compounds Synthesis and Biological Activity of 2-Amino- and 2-aryl (Heteryl) Substituted 1,3-Benzothiazin-4-ones
Mini-Reviews in Medicinal Chemistry Vaccine Delivery - Current Trends and Future
Current Drug Delivery BMI1 Regulation of Self-Renewal and Multipotency in Human Mesenchymal Stem Cells
Current Stem Cell Research & Therapy Role of Moving Average Analysis for Development of Multi-Target (Q)SAR Models
Mini-Reviews in Medicinal Chemistry Benzocaine: Review on a Drug with Unfold Potential
Mini-Reviews in Medicinal Chemistry Glycolipids as Immune Modulatory Tools
Mini-Reviews in Medicinal Chemistry Bacterial Eukaryotic Type Serine-Threonine Protein Kinases: From Structural Biology to Targeted Anti-Infective Drug Design
Current Topics in Medicinal Chemistry Quinoxaline Derivatives: Novel and Selective Butyrylcholinesterase Inhibitors
Medicinal Chemistry An Improved Computational Prediction Model for Lysine Succinylation Sites Mapping on Homo sapiens by Fusing Three Sequence Encoding Schemes with the Random Forest Classifier
Current Genomics Current Strategies in TB Immunotherapy
Current Molecular Medicine Antibiotic Use in Children - Off-Label Use
Current Drug Targets Meet Our Editorial Board Member
The Natural Products Journal Structure-Based Drug Discovery Accelerated by Many-Core Devices
Current Drug Targets Bifunctional Anti-HIV/TB Inhibitors: Perspective from In-Silico Design and Molecular Dynamics Simulations
Letters in Drug Design & Discovery Pleuroparenchymal Fibroelastosis: Its Pathological Characteristics
Current Respiratory Medicine Reviews Anti-Mycobacterium tuberculosis Activity of Calophyllum brasiliense Extracts Obtained by Supercritical Fluid Extraction and Conventional Techniques
Current Pharmaceutical Biotechnology Intracellular Drug Delivery: Mechanisms for Cell Entry
Current Pharmaceutical Design Prospective Observation for Seven-Year's Highly Active Antiretroviral Therapy in Chinese HIV-1 Infected Patients
Current HIV Research Αlpha-2 Adrenergic and Opioids Receptors Participation in Mice Gastroprotection of Abelmoschus esculentus Lectin
Current Pharmaceutical Design