摘要
一组重要的止吐药物,用于治疗化疗后的恶心和呕吐,其结构中含有吲哚部分,作为5-羟色胺3型血清素受体拮抗剂(5- ht3)。本研究重点研究具有5-HT3受体拮抗剂活性的吲哚核心化合物,这些化合物已被成功用于癌症治疗过程中减少化疗不良反应的止吐药物。讨论了它们的合成、生物活性和一些突出的特性,为开发更有效的止吐药物提供了一般性的展望。
关键词: 止吐药,5-HT3,吲哚,合成,恩丹司琼,雷莫司琼,多拉司琼,格拉司琼,瑞卡司琼,托司琼…
Current Medicinal Chemistry
Title:Synthesis and Development of Indole Based 5-HT3 Receptor Antagonists as Anti-Emetic Drugs in Oncology: An Update
Volume: 28 Issue: 42
关键词: 止吐药,5-HT3,吲哚,合成,恩丹司琼,雷莫司琼,多拉司琼,格拉司琼,瑞卡司琼,托司琼…
摘要: An important group of antiemetic drugs used in the treatment of nausea and vomiting after chemotherapy containing an indole moiety in their structures, working as 5- hydroxytryptamine type 3 serotonin receptor antagonist (5-HT3). This study focuses on compounds bearing an indole core that present a 5-HT3 receptor antagonist activity, which have been successfully used as antiemetic drugs for reducing chemotherapy adverse secondary effects during cancer treatment. Their synthesis, biological activities, and some outstanding characteristics are discussed, providing a general outlook towards the development of more efficient antiemetic drugs.
Export Options
About this article
Cite this article as:
Synthesis and Development of Indole Based 5-HT3 Receptor Antagonists as Anti-Emetic Drugs in Oncology: An Update, Current Medicinal Chemistry 2021; 28 (42) . https://dx.doi.org/10.2174/0929867328666210708091134
DOI https://dx.doi.org/10.2174/0929867328666210708091134 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
- 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
-
Meet Our Editorial Board Member:
Current Drug Targets Bridging the Gap Between Chemistry and Biotechnology - Large Molecules with Potential, How Could Biotechnology Complement Chemistry?
Current Organic Chemistry (Section A: Molecular, Structural, and Cellular Biology of Drug Transporters) The Role of MDR1 Genetic Polymorphisms in Interindividual Variability in P-glycoprotein Expression and Function
Current Drug Metabolism Non-IgE Mediated Food Allergy – Update of Recent Progress in Mucosal Immunity
Inflammation & Allergy - Drug Targets (Discontinued) Imaging of HER-2 Overexpression in Tumors for Guiding Therapy
Current Pharmaceutical Design Molecules of Parasites as Immunomodulatory Drugs
Current Topics in Medicinal Chemistry Pharmacophore, 3D-QSAR Models and Dynamic Simulation of 1,4-Benzothiazines for Colorectal Cancer Treatment
Combinatorial Chemistry & High Throughput Screening Generation of Bispecific Antibodies by Fc Heterodimerization and their Application
Current Pharmaceutical Biotechnology Anti-Inflammatory and Pro-Resolving Effects of N-3 PUFA in Cancers: Structures and Mechanisms
Current Topics in Medicinal Chemistry Defensins: Key Molecules in Ocular Surface Protection
Current Immunology Reviews (Discontinued) Potential Crossreactivity of Human Immune Responses Against HCMV Glycoprotein B
Current Drug Discovery Technologies Advances in Chemotherapy and Targeted Systemic Therapies for Urothelial Cancer
Current Drug Therapy Role of Antioxidants, Essential Fatty Acids, Carnitine, Vitamins, Phytochemicals and Trace Elements in the Treatment of Diabetes Mellitus and its Chronic Complications
Endocrine, Metabolic & Immune Disorders - Drug Targets Structure and Expression of Different Serum Amyloid A (SAA) Variants and their Concentration-Dependent Functions During Host Insults
Current Medicinal Chemistry Abundance and Diversity of GI Microbiota Rather than IgG<sub>4</sub> Levels Correlate with Abdominal Inconvenience and Gut Permeability in Consumers Claiming Food Intolerances
Endocrine, Metabolic & Immune Disorders - Drug Targets Chemotherapy-Induced Modifications to Gastrointestinal Microflora: Evidence and Implications of Change
Current Drug Metabolism Use of Gadoxetic Acid-enhanced MRI to Predict the Development of Postoperative Pancreatic Fistulas by Estimating the Degree of Pancreatic Fibrosis
Current Medical Imaging miR-21, An Oncogenic Target miRNA for Cancer Therapy: Molecular Mechanisms and Recent Advancements in Chemo and Radio-resistance
Current Gene Therapy Proteinase-Activated Receptor-2: Physiological and Pathophysiological Roles
Current Medicinal Chemistry - Cardiovascular & Hematological Agents MR Imaging Findings of Uterine Cervical Carcinoma
Current Medical Imaging