Abstract
A novel series of Mannich bases of 1, 3-dihydroxyxanthone derivatives were designed and synthesized. The chemical structures of the compounds were characterized by IR, MS and NMR spectra. Their in vitro toxicities on six tumor cell lines including NCI-H460 (lung cancer), TCA-8113 (tongue squamous cell carcinomas), BEL-7402 (liver cancer), HepG2 (hepatocarcinoma), SGC-7901 (gastric carcinoma) and T24 (urinary bladder carcinoma) were studied through MTT assay. The results showed that most of the compounds displayed mild to good inhibitory activities on the cancer cell lines. Some preliminary structure-activity relationships were also discussed.
Keywords: Xanthone derivatives, Synthesis, Mannich bases, Antitumor activity, Structure-activity relationships, MTT assay.
Letters in Drug Design & Discovery
Title:Synthesis and Biological Evaluation of 1, 3-Dihydroxyxanthone Mannich Base Derivatives as Potential Antitumor Agents
Volume: 10 Issue: 8
Author(s): Wenli Lan, Jingchen Wei, Jiangke Qin, Zhengmin Yang, Guifa Su and Zhikai Dai
Affiliation:
Keywords: Xanthone derivatives, Synthesis, Mannich bases, Antitumor activity, Structure-activity relationships, MTT assay.
Abstract: A novel series of Mannich bases of 1, 3-dihydroxyxanthone derivatives were designed and synthesized. The chemical structures of the compounds were characterized by IR, MS and NMR spectra. Their in vitro toxicities on six tumor cell lines including NCI-H460 (lung cancer), TCA-8113 (tongue squamous cell carcinomas), BEL-7402 (liver cancer), HepG2 (hepatocarcinoma), SGC-7901 (gastric carcinoma) and T24 (urinary bladder carcinoma) were studied through MTT assay. The results showed that most of the compounds displayed mild to good inhibitory activities on the cancer cell lines. Some preliminary structure-activity relationships were also discussed.
Export Options
About this article
Cite this article as:
Lan Wenli, Wei Jingchen, Qin Jiangke, Yang Zhengmin, Su Guifa and Dai Zhikai, Synthesis and Biological Evaluation of 1, 3-Dihydroxyxanthone Mannich Base Derivatives as Potential Antitumor Agents, Letters in Drug Design & Discovery 2013; 10 (8) . https://dx.doi.org/10.2174/15701808113100890029
DOI https://dx.doi.org/10.2174/15701808113100890029 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
-
Outline of Proteins and Signaling Pathways Involved in Heart Failure
Current Protein & Peptide Science Bortezomib Enhances the Antitumor Effects of Interferon-β Gene Transfer on Melanoma Cells
Anti-Cancer Agents in Medicinal Chemistry Chemokines and Breast Cancer: A Gateway to Revolutionary Targeted Cancer Treatments?
Current Medicinal Chemistry Lentiviral-Mediated Overexpression of MicroRNA-141 Promotes Cell Proliferation and Inhibits Apoptosis in Human Esophageal Squamous Cell Carcinoma
Recent Patents on Anti-Cancer Drug Discovery Genome-Wide Integrated Analyses of Androgen Receptor Signaling in Prostate Cancer Based on High-Throughput Technology
Current Drug Targets Immunological and Translational Aspects of Glycolytic Metabolism in Various Human Tumor Entities
Clinical Immunology, Endocrine & Metabolic Drugs (Discontinued) Formulation Considerations of Gadolinium Lipid Nanoemulsion for Intravenous Delivery to Tumors in Neutron-Capture Therapy
Current Drug Delivery The Molecular Machinery Regulating Apoptosis Signal Transduction and its Implication in Human Physiology and Pathophysiologies
Current Molecular Medicine Evidence of PKC Binding and Translocation to Explain the Anticancer Mechanism of Chlorogenic Acid in Breast Cancer Cells
Current Molecular Medicine The Quest for a Tumor Suppressor Gene Phenotype
Current Molecular Medicine The c-Met Inhibitors: A New Class of Drugs in the Battle Against Advanced Nonsmall- Cell Lung Cancer
Current Pharmaceutical Design Optical Diagnosis of Head and Neck Cancers (Review)
Reviews on Recent Clinical Trials Endoglin-Targeted Cancer Therapy
Current Drug Delivery Chemopreventive Agents Alters Global Gene Expression Pattern: Predicting their Mode of Action and Targets
Current Cancer Drug Targets Eosinophils in Cancer: Favourable or Unfavourable?
Current Medicinal Chemistry Specific Targeting of HER2-Positive Head and Neck Squamous Cell Carcinoma Line HN5 by Idarubicin-ZHER2 Affibody Conjugate
Current Cancer Drug Targets Immunomodulation Mechanism of Antidepressants: Interactions between Serotonin/Norepinephrine Balance and Th1/Th2 Balance
Current Neuropharmacology Nanopotentiation of Propolis for Revocation of Enzyme Imbalance in UVB Induced Cutaneous Toxicity in Murine Model: a Preliminary Study for Chemoprotection of Skin Cancer
Drug Delivery Letters Targeted Regulation of PI3K/Akt/mTOR/NF-κB Signaling by Indole Compounds and their Derivatives: Mechanistic Details and Biological Implications for Cancer Therapy
Anti-Cancer Agents in Medicinal Chemistry Analogs of Cinnamic Acid Benzyl Amide As Nonclassical Inhibitors of Activated JAK2 Kinase
Current Cancer Drug Targets