Abstract
Based on the structure of 23-hydroxybetulinic acid (1), a series of 28-amide derivatives were synthesized. Biological evaluation in vitro for their antitumor activities against five cell lines (A549, BEL-7402, SF-763, B16 and HL-60) has indicated that compound 6g possesses the most effective antitumor activity with an IC50 value of 10.47 μM when treated with HL-60 cells. In vivo testing has also shown a comparable activity of 6g to cyclophosphamide against H22 liver tumor in mice and 5-fluorouracil against B16 melanoma, respectively.
Keywords: 23-hydroxy betulinic acid, 28-carboxylic acid, amide derivatives, antitumor activity.
Medicinal Chemistry
Title:Synthesis and Biological Activity of 28-Amide Derivatives of 23-Hydroxy Betulinic Acid as Antitumor Agent Candidates
Volume: 9 Issue: 7
Author(s): Yi Bi, Jinyi Xu, Fei Sun, Xiaoming Wu, Wencai Ye, Yijun Sun and Wenwen Huang
Affiliation:
Keywords: 23-hydroxy betulinic acid, 28-carboxylic acid, amide derivatives, antitumor activity.
Abstract: Based on the structure of 23-hydroxybetulinic acid (1), a series of 28-amide derivatives were synthesized. Biological evaluation in vitro for their antitumor activities against five cell lines (A549, BEL-7402, SF-763, B16 and HL-60) has indicated that compound 6g possesses the most effective antitumor activity with an IC50 value of 10.47 μM when treated with HL-60 cells. In vivo testing has also shown a comparable activity of 6g to cyclophosphamide against H22 liver tumor in mice and 5-fluorouracil against B16 melanoma, respectively.
Export Options
About this article
Cite this article as:
Bi Yi, Xu Jinyi, Sun Fei, Wu Xiaoming, Ye Wencai, Sun Yijun and Huang Wenwen, Synthesis and Biological Activity of 28-Amide Derivatives of 23-Hydroxy Betulinic Acid as Antitumor Agent Candidates, Medicinal Chemistry 2013; 9 (7) . https://dx.doi.org/10.2174/1573406411309070005
DOI https://dx.doi.org/10.2174/1573406411309070005 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...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
-
Targeting Malignancies with Disulfiram (Antabuse): Multidrug Resistance, Angiogenesis, and Proteasome
Current Cancer Drug Targets Interaction of Anthocyanins with Drug-metabolizing and Antioxidant Enzymes
Current Medicinal Chemistry A Novel Class of Emerging Anticancer Compounds: Oxyprenylated Secondary Metabolites from Plants and Fungi
Current Medicinal Chemistry Review on Pharmacological and Phytochemical Prospects of Traditional Medicinal Plant: <i>Persicaria hydropiper</i> (Smartweed)
Current Topics in Medicinal Chemistry Cucurbitacins as Inducers of Cell Death and a Rich Source of Potential Anticancer Compounds
Current Pharmaceutical Design Novel Indications for Benzodiazepine Antagonist Flumazenil in GABA Mediated Pathological Conditions of the Central Nervous System
Current Pharmaceutical Design Innovative Therapeutic Potential of Cannabinoid Receptors as Targets in Alzheimer’s Disease and Less Well-Known Diseases
Current Medicinal Chemistry Extrahepatic Targets and Cellular Reactivity of Drug Metabolites
Current Medicinal Chemistry Intramammary Application of Non-Methylated-CpG Oligodeoxynucleotides (CpG) Inhibits both Local and Systemic Mammary Carcinogenesis in Female BALB/c Her-2/neu Transgenic Mice
Current Cancer Drug Targets Sanguinarine: A Double-Edged Sword of Anticancer and Carcinogenesis and Its Future Application Prospect
Anti-Cancer Agents in Medicinal Chemistry Oxidation Inhibits Iron-Induced Blood Coagulation
Current Drug Targets Do We have the Evidence to Repurpose Levamisole for Treatment of COVID 19?
Current Drug Therapy Apoptosis Signaling Pathways in Anticancer Therapy
Current Cancer Therapy Reviews Oncologic Imaging End-Points for the Assessment of Therapy Response
Recent Patents on Anti-Cancer Drug Discovery Exploring Mechanisms of MicroRNA Downregulation in Cancer
MicroRNA The Role of Phospholipase D Enzyme(s) in Modulating Cell Signaling: Implications for Cancer Drug Development
Current Bioactive Compounds New Insights into Redox-Modulated Cell Signaling
Current Pharmaceutical Design Alteronol Induces Differentiation of Melanoma B16-F0 Cells
Recent Patents on Anti-Cancer Drug Discovery Patented Biomarker Panels in Early Detection of Cancer
Recent Patents on Biomarkers In Vitro Evaluation of Antimicrobial and Antiproliferative Activities for Compounds Isolated from the Ficus Bubu Warb. (Moraceae) Fruits: Chemotaxonomic Significance
Drug Delivery Letters