Abstract
Hypoxia inducible factor-1 (HIF-1) is a key mediator during cancer cells to adapt tumor hypoxic condition. In this study, a series of adamantane-based compounds were synthesized and evaluated as potential inhibitors of HIF-1α. Examination of their structure-activity relationship (SAR) identified the adamantane-containing indole derivative 20a as a potent inhibitor of HIF-1α in Hep3B cell lines under tumor hypoxia (IC50 = 0.02 µM). The study herein may provide valuable information for the development of novel therapeutics against cancer and tumor angiogenesis.
Keywords: Adamantane, hypoxia inducible factor-1, structure-activity relationship, tumor angiogenesis.
Medicinal Chemistry
Title:Design, Synthesis and Structure-Activity Relationship Studies of Novel 4 (1-adamantyl) Phenyl Analogues as HIF-1α Inhibitors
Volume: 12 Issue: 4
Author(s): Yan Xia, Qiong Duan, Bao-Hua Zhao, Dong-Feng Li and Rui-Bin Hou
Affiliation:
Keywords: Adamantane, hypoxia inducible factor-1, structure-activity relationship, tumor angiogenesis.
Abstract: Hypoxia inducible factor-1 (HIF-1) is a key mediator during cancer cells to adapt tumor hypoxic condition. In this study, a series of adamantane-based compounds were synthesized and evaluated as potential inhibitors of HIF-1α. Examination of their structure-activity relationship (SAR) identified the adamantane-containing indole derivative 20a as a potent inhibitor of HIF-1α in Hep3B cell lines under tumor hypoxia (IC50 = 0.02 µM). The study herein may provide valuable information for the development of novel therapeutics against cancer and tumor angiogenesis.
Export Options
About this article
Cite this article as:
Xia Yan, Duan Qiong, Zhao Bao-Hua, Li Dong-Feng and Hou Rui-Bin, Design, Synthesis and Structure-Activity Relationship Studies of Novel 4 (1-adamantyl) Phenyl Analogues as HIF-1α Inhibitors, Medicinal Chemistry 2016; 12 (4) . https://dx.doi.org/10.2174/1573406412666151109113007
DOI https://dx.doi.org/10.2174/1573406412666151109113007 |
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
-
Control of Tumor Markers Using Nanotechnology
Mini-Reviews in Medicinal Chemistry Toxicological Profile of Therapeutic Nanodelivery Systems
Current Drug Metabolism Synthesis and Antiproliferative Evaluation of Hybrids of Indolin-2-one and Quinazoline-4(3H)-one Linked via Imine Bond
Letters in Drug Design & Discovery Emerging Therapy for Diabetic Neuropathy: Cell Therapy Targeting Vessels and Nerves
Endocrine, Metabolic & Immune Disorders - Drug Targets A Sustainable Approach to Bis-Indole Synthesis Using Propylene Carbonate as an Eco-Friendly Solvent
Current Organic Synthesis Recent Advancement in Discovery and Development of Natural Product Combretastatin-inspired Anticancer Agents
Anti-Cancer Agents in Medicinal Chemistry Proteinases as Biomarkers in Breast Cancer Prognosis and Diagnosis
Mini-Reviews in Medicinal Chemistry The Use of PET for Radiotherapy
Current Medical Imaging Evaluation of Cytotoxic Mechanisms of Clinacanthus Nutans Extracts in Cancer Cells
The Natural Products Journal Oncogenic MicroRNA-27a is a Target for Genistein in Ovarian Cancer Cells
Anti-Cancer Agents in Medicinal Chemistry Safety of Systemic Biologic Agents in the Treatment of Non-malignant Skin Disorders
Current Drug Safety Mannosylated Solid Lipid Nanocarriers of Chrysin to Target Gastric Cancer: Optimization and Cell Line Study
Current Drug Delivery Pluripotency and Targeted Reprogramming: Strategies, Disease Modeling and Drug Screening
Current Drug Delivery Meet Our Editorial Board Member:
Applied Clinical Research, Clinical Trials and Regulatory Affairs Structural and Bioactive Studies of Halogenated Constituents from Sponges
Current Medicinal Chemistry Colloidal Nanocarriers as Versatile Targeted Delivery Systems for Cervical Cancer
Current Pharmaceutical Design ThermoTRP Channels in Nociceptors: Taking a Lead from Capsaicin Receptor TRPV1
Current Neuropharmacology The Important Roles of miR-205 in Normal Physiology, Cancers and as a Potential Therapeutic Target
Current Cancer Drug Targets P-Selectin Glycoprotein Ligand-1 as a Potential Target for Humoral Immunotherapy of Multiple Myeloma (Supplementry Material)
Current Cancer Drug Targets Nanostructured Lipid Carriers (NLCs) for Drug Delivery: Role of Liquid Lipid (Oil)
Current Drug Delivery