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
-
Recent Advances in PUVA Photochemotherapy and PDT for the Treatment of Cancer
Current Pharmaceutical Design Particulate Systems as Adjuvants and Carriers for Peptide and Protein Antigens
Current Drug Delivery Organic Toxins as Tools to Understand Ion Channel Mechanisms and Structure
Current Topics in Medicinal Chemistry subject Index To Volume 2
Current Protein & Peptide Science Genotypic Characterization of Vancomycin-Resistant Enterococcus spp. In Tertiary Center, Iran
Infectious Disorders - Drug Targets HIV-1 Vpr: A Closer Look at the Multifunctional Protein from the Structural Perspective
Current HIV Research Meet Our Associate Editor
Anti-Cancer Agents in Medicinal Chemistry Synthesis and Biological Evaluation of Curcumin-Nitroxide-Based Molecular Hybrids as Antioxidant and Anti-Proliferative Agents
Medicinal Chemistry Applications and Case Studies of the Next-Generation Sequencing Technologies in Food, Nutrition and Agriculture
Recent Patents on Food, Nutrition & Agriculture Induction of Oral Tolerance with Transgenic Plants Expressing Antigens for Prevention/Treatment of Autoimmune, Allergic and Inflammatory Diseases
Current Pharmaceutical Biotechnology Quinolone-Based Drugs Against Toxoplasma gondii and Plasmodium spp
Current Drug Targets - Infectious Disorders Indole and Indoline Scaffolds in Antimicrobials: Overview, Synthesis and Recent Advances in Antimicrobial Research
Current Medicinal Chemistry Intestinal Fibrosis in Crohns Disease: Medical Treatment or Surgery?
Current Drug Targets An Integrated Re-Annotation Approach for Functional Predictions of Hypothetical Proteins in Microbial Genomes
Current Bioinformatics Efficient Antibacterial Agents: A Review of the Synthesis, Biological Evaluation and Mechanism of Pleuromutilin Derivatives
Current Topics in Medicinal Chemistry Regulation of Cell Wall Synthesis and Growth
Current Molecular Medicine Epidemiology and Management of Infectious Complications in Contemporary Management of Chronic Leukemias
Infectious Disorders - Drug Targets Small Molecules for the Activation of Human γ δ T Cell Responses Against Infection
Recent Patents on Anti-Infective Drug Discovery Morbidity and Mortality Associated with Pharmacotherapy. Evolution and Current Concept of Drug-Related Problems
Current Pharmaceutical Design Anti-VEGF Therapy for Retinal Vein Occlusions
Current Drug Targets