Abstract
A novel tamibarotene derivative was synthesized by coupling cytotoxic agent 5-Fluorouracil (5-FU) with tamibarotene via ester. This hybrid drug (compound 10) was evaluated for its antiproliferative activities against human leukemic U937, HL-60 and K562 cell lines in vitro. Results showed that compound 10 exhibited more potent anti-leukemic activity than the positive control tamibarotene. Furthermore, the preliminary stability test of compound 10 revealed that it could release tamibarotene and 5-FU significantly in vitro. These interesting results would be meaningful to develop more potent drugs for the treatment of human leukemia.
Keywords: Tamibarotene (AM80), multitarget, 5-fluorouracil (5-FU), anticancer, leukemia.
Letters in Drug Design & Discovery
Title:Design, Synthesis and Biological Evaluation of Novel Tamibarotene Derivative as Multitarget Anticancer Agent
Volume: 13 Issue: 8
Author(s): Yuqi Jiang, Jinning Hou, Xiaoyang Li, Wenfang Xu and Yingjie Zhang
Affiliation:
Keywords: Tamibarotene (AM80), multitarget, 5-fluorouracil (5-FU), anticancer, leukemia.
Abstract: A novel tamibarotene derivative was synthesized by coupling cytotoxic agent 5-Fluorouracil (5-FU) with tamibarotene via ester. This hybrid drug (compound 10) was evaluated for its antiproliferative activities against human leukemic U937, HL-60 and K562 cell lines in vitro. Results showed that compound 10 exhibited more potent anti-leukemic activity than the positive control tamibarotene. Furthermore, the preliminary stability test of compound 10 revealed that it could release tamibarotene and 5-FU significantly in vitro. These interesting results would be meaningful to develop more potent drugs for the treatment of human leukemia.
Export Options
About this article
Cite this article as:
Jiang Yuqi, Hou Jinning, Li Xiaoyang, Xu Wenfang and Zhang Yingjie, Design, Synthesis and Biological Evaluation of Novel Tamibarotene Derivative as Multitarget Anticancer Agent, Letters in Drug Design & Discovery 2016; 13 (8) . https://dx.doi.org/10.2174/157018081308160826182531
DOI https://dx.doi.org/10.2174/157018081308160826182531 |
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
-
Regeneration of the Gastric Mucosa and its Glands from Stem Cells
Current Medicinal Chemistry Nucleic Acid Aptamers Against Protein Kinases
Current Medicinal Chemistry Therapeutic Potential of Targeting TREM-1 in Inflammatory Diseases and Cancer
Current Pharmaceutical Design Inhibitors of the HSP90 Molecular Chaperone: Attacking the Master Regulator in Cancer
Current Topics in Medicinal Chemistry Diagnoses of Gastrointestinal Cancers After Gastrointestinal Bleeding in Patients Receiving Clopidogrel or Warfarin
Current Drug Safety Epigenetic and miRNAs Dysregulation in Prostate Cancer: The role of Nutraceuticals
Anti-Cancer Agents in Medicinal Chemistry Pharmacological Interference With Protein-protein Interactions of Akinase Anchoring Proteins as a Strategy for the Treatment of Disease
Current Drug Targets Spectral Imaging Technology - A Review on Skin and Endoscopy Applications
Recent Patents on Medical Imaging Tumor-Associated Macrophages as Potential Targets for Anti-Cancer Activity of Marine Invertebrate-Derived Compounds
Current Pharmaceutical Design Antibiotic Properties and Applications of Lactoferrin
Current Pharmaceutical Design Natural Sesquiterpenoids as Cytotoxic Anticancer Agents
Mini-Reviews in Medicinal Chemistry Histone Deacetylase Inhibitors: A Review on Class-I Specific Inhibition
Mini-Reviews in Medicinal Chemistry Roles of Interferon Induced Protein with Tetratricopeptide Repeats (IFIT) Family in Cancer
Current Medicinal Chemistry Irreversible LSD1 Inhibitors: Application of Tranylcypromine and Its Derivatives in Cancer Treatment
Current Topics in Medicinal Chemistry CXCR4 Receptor as a Promising Target for Oncolytic Drugs
Mini-Reviews in Medicinal Chemistry Chemotherapy in Addition to Preoperative Radiotherapy in Locally Advanced Rectal Cancer – A Systematic Overview
Reviews on Recent Clinical Trials Functional Food: Product Development and Health Benefits
Recent Patents on Engineering Polysaccharide Based Formulations for Mucosal Drug Delivery: A Review
Current Pharmaceutical Design The Competence of 7,8-Diacetoxy-4-Methylcoumarin and Other Polyphenolic Acetates in Mitigating the Oxidative Stress and their Role in Angiogenesis
Current Topics in Medicinal Chemistry Targeting Tumor Lymphangiogenesis: An Update
Current Medicinal Chemistry