Abstract
On the basis of harmine and 1-methoxy-canthin-6-one chemical structures, a series of novel 1,4-disubstituted and 1,4,9-trisubstituted β-carbolines and tetracyclic derivatives were designed and synthesized. Cytotoxic activities of these compounds in vitro were investigated in a human tumor cell line panel. Almost all compounds demonstrated interesting cytotoxic activities in particular against prostate cancer cells PC-3 with IC50 in the low micromolar range. Compound X was found to be the most potent one with IC50 value of 8.0 μM; this suggests further studies with models of prostate cancer.
Keywords: β-carbolines, 1-methoxycanthin-6-one, prostate cancer, harmine, Cytotoxic, 1,4,9-trisubstituted, 1,4-disubstituted, alkaloids, herbal drug, antitumor
Mini-Reviews in Medicinal Chemistry
Title: Synthesis and Cytotoxic Activity of New β-Carboline Derivatives
Volume: 11 Issue: 6
Author(s): A. Peduto, V. More, P. de Caprariis, M. Festa, A. Capasso, S. Piacente, L. De Martino, V. De Feo and R. Filosa
Affiliation:
Keywords: β-carbolines, 1-methoxycanthin-6-one, prostate cancer, harmine, Cytotoxic, 1,4,9-trisubstituted, 1,4-disubstituted, alkaloids, herbal drug, antitumor
Abstract: On the basis of harmine and 1-methoxy-canthin-6-one chemical structures, a series of novel 1,4-disubstituted and 1,4,9-trisubstituted β-carbolines and tetracyclic derivatives were designed and synthesized. Cytotoxic activities of these compounds in vitro were investigated in a human tumor cell line panel. Almost all compounds demonstrated interesting cytotoxic activities in particular against prostate cancer cells PC-3 with IC50 in the low micromolar range. Compound X was found to be the most potent one with IC50 value of 8.0 μM; this suggests further studies with models of prostate cancer.
Export Options
About this article
Cite this article as:
Peduto A., More V., de Caprariis P., Festa M., Capasso A., Piacente S., De Martino L., De Feo V. and Filosa R., Synthesis and Cytotoxic Activity of New β-Carboline Derivatives, Mini-Reviews in Medicinal Chemistry 2011; 11 (6) . https://dx.doi.org/10.2174/138955711795843383
DOI https://dx.doi.org/10.2174/138955711795843383 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
Related Articles
-
<i>In Vitro</i> Anti-proliferative Properties of Flavonoids Isolated from <i>Artocarpus Heterophyllus</i> on Cancer Cell Lines
The Natural Products Journal Therapeutics Interventions with Anti-Inflammatory Creams in Post Radiation Acute Skin Reactions: A Systematic Review of Most Important Clinical Trials
Recent Patents on Inflammation & Allergy Drug Discovery Laccases in Pharmaceutical Chemistry: A Comprehensive Appraisal
Mini-Reviews in Organic Chemistry Prostate-Specific G-Protein Coupled Receptor, an Emerging Biomarker Regulating Inflammation and Prostate Cancer Invasion
Current Molecular Medicine Pharmacological Benefits of Active Components of Natural Products Against Traumatic Brain Injury - A Review
Current Pharmacogenomics and Personalized Medicine Angiogenesis Inhibitors: Implications for Combination with Conventional Therapies
Current Pharmaceutical Design Recent Advances and Approaches in Targeting Apoptosis Signaling Pathways for Anti-Cancer Therapeutics
Current Cancer Therapy Reviews Nuclear Medicine: Proof of Principle for Targeted Drugs in Diagnosis and Therapy
Current Pharmaceutical Design Novel Approaches for Molecular Targeted Therapy of Breast Cancer: Interfering with PI3K/AKT/mTOR Signaling
Current Cancer Drug Targets Impact on DNA Methylation in Cancer Prevention and Therapy by Bioactive Dietary Components
Current Medicinal Chemistry Growth Restriction: Etiology, Maternal and Neonatal Outcome. A Review
Current Women`s Health Reviews Targeting the Ubiquitin Proteasome System: Beyond Proteasome Inhibition
Current Pharmaceutical Design The Interaction of NK Cells and Dendritic Cells in the Tumor Environment: How to Enforce NK Cell & DC Action Under Immunosuppressive Conditions?
Current Medicinal Chemistry Cytotoxic Tumor-Targeting Peptides From In Vivo Phage Display
Combinatorial Chemistry & High Throughput Screening Epstein-Barr Virus-associated Gastric Cancer and Potential Mechanisms of Oncogenesis
Current Cancer Drug Targets Sperm Quality in Mouse After Exposure to Low Doses of TCDD
Current Topics in Medicinal Chemistry S100A8 and S100A9 Overexpression Is Associated with Poor Pathological Parameters in Invasive Ductal Carcinoma of the Breast
Current Cancer Drug Targets Controlled-release Particulate Cytokine Adjuvants for Cancer Therapy
Endocrine, Metabolic & Immune Disorders - Drug Targets Discovery and Applications of Disulfide-Rich Cyclic Peptides
Current Topics in Medicinal Chemistry Biophysical Characterization of Glycodendrimers As Nano-carriers for HIV Peptides
Current Medicinal Chemistry