Abstract
Histone deacetylases (HDACs) inhibitors have multiple effects targeting the cancer cells and have become one of the promising cancer therapeutics with possibly broad applicability. Combination of HDAC inhibitors with the cytotoxic fluorouracil (5-FU) showed additive and synergistic effects both in vitro and in vivo. To explore the possibility in cancer therapy of a bivalent agent that combines two bioactive groups within a single molecular architecture, we designed and synthesized new dual-acting compounds by combining the bioactive fragment of MS-275, a clinical HDACs inhibitor, with cytotoxic agent 5-FU. The target compounds 9a and 9b showed comparable HDACs inhibition with MS-275 and moderate antiproliferative acitivities against six cancer cells lines.
Keywords: Anticancer, HDAC, MS-275, Multitarget, 5-Fluorouracil.
Medicinal Chemistry
Title:Discovery of Multi-target Anticancer Agents Based on HDAC Inhibitor MS-275 and 5-FU
Volume: 12 Issue: 1
Author(s): Yuqi Jiang, Xiaoguang Li, Xiaoyang Li, Jinning Hou, Yongzheng Ding, Jian Zhang, Wenfang Xu and Yingjie Zhang
Affiliation:
Keywords: Anticancer, HDAC, MS-275, Multitarget, 5-Fluorouracil.
Abstract: Histone deacetylases (HDACs) inhibitors have multiple effects targeting the cancer cells and have become one of the promising cancer therapeutics with possibly broad applicability. Combination of HDAC inhibitors with the cytotoxic fluorouracil (5-FU) showed additive and synergistic effects both in vitro and in vivo. To explore the possibility in cancer therapy of a bivalent agent that combines two bioactive groups within a single molecular architecture, we designed and synthesized new dual-acting compounds by combining the bioactive fragment of MS-275, a clinical HDACs inhibitor, with cytotoxic agent 5-FU. The target compounds 9a and 9b showed comparable HDACs inhibition with MS-275 and moderate antiproliferative acitivities against six cancer cells lines.
Export Options
About this article
Cite this article as:
Jiang Yuqi, Li Xiaoguang, Li Xiaoyang, Hou Jinning, Ding Yongzheng, Zhang Jian, Xu Wenfang and Zhang Yingjie, Discovery of Multi-target Anticancer Agents Based on HDAC Inhibitor MS-275 and 5-FU, Medicinal Chemistry 2016; 12 (1) . https://dx.doi.org/10.2174/1573406411666150714111045
DOI https://dx.doi.org/10.2174/1573406411666150714111045 |
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
-
A Dual Role of Cyclin E in Cell Proliferation and Apotosis May Provide a Target for Cancer Therapy
Current Cancer Drug Targets Stem Cells and the Side Population Theory: A Critical Review
Current Tissue Engineering (Discontinued) HCV-Related Transformation and New Therapeutic Strategies: An Update
Current Cancer Therapy Reviews PI3K/Akt Signalling Pathway Specific Inhibitors: A Novel Strategy to Sensitize Cancer Cells to Anti-Cancer Drugs
Current Pharmaceutical Design Editorial (Hot Topic: Innovative Approaches for the Management of Pediatric Malignancies)
Current Medicinal Chemistry Relationships between Serotoninergic System and Skin Fibrotic
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Multidrug Transporters as Drug Targets
Current Drug Targets Targeted Taxane Delivery Systems: Recent Advances
Drug Delivery Letters Targeting the Acute Myeloid Leukemia Stem Cells
Anti-Cancer Agents in Medicinal Chemistry High-Risk Neuroblastoma: Poor Outcomes Despite Aggressive Multimodal Therapy
Current Cancer Therapy Reviews Histone Deacetylase Inhibitors: A New Wave of Molecular Targeted Anticancer Agents
Recent Patents on Anti-Cancer Drug Discovery Systems Medicine Approaches to Improving Understanding, Treatment, and Clinical Management of Neuroendocrine Prostate Cancer
Current Pharmaceutical Design Self-Renewal Versus Differentiation in Hematopoietic Stem and Progenitor Cells: A Focus on Asymmetric Cell Divisions
Current Stem Cell Research & Therapy Immune Modulation of Asian Folk Herbal Medicines and Related Chemical Components for Cancer Management
Current Medicinal Chemistry Designing of Novel Carbonic Anhydrase Inhibitors and Activators
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Class II Phosphoinositide 3-Kinases as Potential Novel Drug Targets
Current Signal Transduction Therapy Adverse Effects and Drug Interactions of Biologic Agents
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Clinical and Genetic Features of Warts, Hypogammaglobulinemia, Infections and Myelokathexis (WHIM) Syndrome
Current Molecular Medicine Anthracyclines Still Prove Effective in Anticancer Therapy
Mini-Reviews in Medicinal Chemistry Nuclear Medicine: Proof of Principle for Targeted Drugs in Diagnosis and Therapy
Current Pharmaceutical Design