Abstract
A series of di-substituted cinnamic hydroxamic derivatives was designed, synthesized and evaluated as HDAC inhibitors. Compound 5f (HS270) demonstrated potent HDAC inhibitory and antiproliferative activities. In xenograft model, 5f showed significant antitumor efficacy in tumorbearing mice.
Keywords: Antitumor, cinnamic, design, histone deacetylase, HDAC, hydroxamaic acid.
Graphical Abstract
Letters in Drug Design & Discovery
Title:Discovery of Novel HDAC Inhibitors by Structure-based Optimization of Cinnamic Hydroxamic Scaffold
Volume: 12 Issue: 5
Author(s): Chengqing Ning, Wenyuan Huang, Wen Wu, Cheng Lu, Yujun He, Lei Yao, Lifei Liu, Xiaohe Zhen, Xiaoyu Liu and Niefang Yu
Affiliation:
Keywords: Antitumor, cinnamic, design, histone deacetylase, HDAC, hydroxamaic acid.
Abstract: A series of di-substituted cinnamic hydroxamic derivatives was designed, synthesized and evaluated as HDAC inhibitors. Compound 5f (HS270) demonstrated potent HDAC inhibitory and antiproliferative activities. In xenograft model, 5f showed significant antitumor efficacy in tumorbearing mice.
Export Options
About this article
Cite this article as:
Ning Chengqing, Huang Wenyuan, Wu Wen, Lu Cheng, He Yujun, Yao Lei, Liu Lifei, Zhen Xiaohe, Liu Xiaoyu and Yu Niefang, Discovery of Novel HDAC Inhibitors by Structure-based Optimization of Cinnamic Hydroxamic Scaffold, Letters in Drug Design & Discovery 2015; 12 (5) . https://dx.doi.org/10.2174/1570180811666141024004832
DOI https://dx.doi.org/10.2174/1570180811666141024004832 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
Related Journals
Related Books
- 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
-
Prospects of Embryonic Stem Cells in Treatment of Hematopoietic Disorders
Current Pharmaceutical Biotechnology Editorial [Hot Topic: Overview of Antiangiogenic Therapies in Hematological Malignancies (Guest Editor: D. Ribatti)]
Current Cancer Drug Targets Cancer Metastasis, a Clinical Dilemma for Therapeutics
Current Drug Therapy Use of a Weighted, Automated Analysis of the Differential Blood Count to Differentiate Sepsis from Non-Infectious Systemic Inflammation: The Intensive Care Infection Score (ICIS)
Inflammation & Allergy - Drug Targets (Discontinued) The Role of 5-Hydroxymethylcytosine in Aging and Alzheimer’s Disease: Current Status and Prospects for Future Studies
Current Alzheimer Research New Therapies to Modulate Post-Infarction Inflammatory Alterations in the Myocardium: State of the Art and Forthcoming Applications
Current Radiopharmaceuticals Physiology of Folic Acid in Health and Disease
Current Drug Metabolism Biochemical Strategies to Anticoagulation: A Comparative Overview
Current Vascular Pharmacology Recent Development in Nano-Sized Dosage Forms of Plant Alkaloid Camptothecin-Derived Drugs
Recent Patents on Anti-Cancer Drug Discovery Haploidentical Stem Cell Transplantation in Childhood
Current Cancer Therapy Reviews Analysis of Simple Sequence Repeats in Mammalian Cell Cycle Genes
Recent Advances in DNA & Gene Sequences (Discontinued) Recent Progress and Related Patents on the Applications of Bone Marrow-Derived Stem/Progenitor Cells in Regenerative Medicine and Cancer Therapies
Recent Patents on Regenerative Medicine A Combined Approach with Rituximab Plus Anti-TRAIL-R Agonistic Antibodies for the Treatment of Haematological Malignancies
Current Pharmaceutical Design A Systematic Review of Drugs in Late-Stage Development for the Treatment of Multiple Sclerosis: A Focus on Oral Synthetic Drugs
Inflammation & Allergy - Drug Targets (Discontinued) Targeting Microtubules to Inhibit Angiogenesis and Disrupt Tumour Vasculature:Implications for Cancer Treatment
Current Cancer Drug Targets Clinical Presentations and Diagnosis of Brucellosis
Recent Patents on Anti-Infective Drug Discovery Neuronal Generation from Somatic Stem Cells: Current Knowledge and Perspectives on the Treatment of Acquired and Degenerative Central Nervous System Disorders
Current Gene Therapy Proteasome Inhibitors and Modulators of Angiogenesis in Multiple Myeloma
Current Medicinal Chemistry 5'-Nucleotidases, Nucleosides and their Distribution in the Brain: Pathological and Therapeutic Implications
Current Medicinal Chemistry Antibody-Drug Conjugate Targets
Current Cancer Drug Targets