Abstract
Four suberoylanilide hydroxamic acid (SAHA) derivatives (N34, N4I, N4B, N24) were designed and synthesized on the basis of our previous studies on N25. Assays for anti-proliferative activity and histone deacetylase (HDAC) activity were performed against human lung cancer (SPC-A-1, LTEP-a-2, NCI-H1650) and normal lung cells (MRC-5), which were compared with those of SAHA. Molecular docking was used to theoretically confirm the receptor-binding ability of N34. Ultimately, N34 was validated as the best HDAC inhibitor candidate. Furthermore, the effects of N34 on the levels of apoptosis- and autophagy-associated proteins caspase-3, caspase-9, Bcl-2 and Beclin-1 in SPC-A-1 cells were evaluated. N34 exerted more evident effects on human lung cancer than the other three SAHA derivatives did.
Keywords: Anti-proliferative activity, apoptosis- and autophagy-associated protein, HDAC activity assay, suberoylanilide hydroxamic acid (SAHA) derivaties, synthesis.
Graphical Abstract
Anti-Cancer Agents in Medicinal Chemistry
Title:Screening Novel SAHA Derivatives as Anti-lung Carcinoma Agents: Synthesis, Biological Evaluation, Docking Studies and Further Mechanism Research between Apoptosis and Autophagyetween Apoptosis and Autophagy
Volume: 15 Issue: 10
Author(s): Weibin Huang, Song Zhang, Zhicheng Yang and Binghong Feng
Affiliation:
Keywords: Anti-proliferative activity, apoptosis- and autophagy-associated protein, HDAC activity assay, suberoylanilide hydroxamic acid (SAHA) derivaties, synthesis.
Abstract: Four suberoylanilide hydroxamic acid (SAHA) derivatives (N34, N4I, N4B, N24) were designed and synthesized on the basis of our previous studies on N25. Assays for anti-proliferative activity and histone deacetylase (HDAC) activity were performed against human lung cancer (SPC-A-1, LTEP-a-2, NCI-H1650) and normal lung cells (MRC-5), which were compared with those of SAHA. Molecular docking was used to theoretically confirm the receptor-binding ability of N34. Ultimately, N34 was validated as the best HDAC inhibitor candidate. Furthermore, the effects of N34 on the levels of apoptosis- and autophagy-associated proteins caspase-3, caspase-9, Bcl-2 and Beclin-1 in SPC-A-1 cells were evaluated. N34 exerted more evident effects on human lung cancer than the other three SAHA derivatives did.
Export Options
About this article
Cite this article as:
Huang Weibin, Zhang Song, Yang Zhicheng and Feng Binghong, Screening Novel SAHA Derivatives as Anti-lung Carcinoma Agents: Synthesis, Biological Evaluation, Docking Studies and Further Mechanism Research between Apoptosis and Autophagyetween Apoptosis and Autophagy, Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (10) . https://dx.doi.org/10.2174/1871520615666150629101107
DOI https://dx.doi.org/10.2174/1871520615666150629101107 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
- 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
-
Molecular Imaging Kits for Hexosamine Biosynthetic Pathway in Oncology
Current Medicinal Chemistry Significance of miR-15a-5p and CNKSR3 as Novel Prognostic Biomarkers in Non-Small Cell Lung Cancer
Anti-Cancer Agents in Medicinal Chemistry Clinical Impact of Hypomethylating Agents in the Treatment of Myelodysplastic Syndromes
Current Pharmaceutical Design The mTOR Pathway: A New Target in Cancer Therapy
Current Cancer Drug Targets Chemotherapy and Target Therapy in the Management of Adult High- Grade Gliomas
Current Cancer Drug Targets Safety and Utilization of Blood Components as Therapeutic Delivery Systems
Current Pharmaceutical Biotechnology Dendrimer Based Formulation of Erlotiniib HCl: Development, Characterization and <i>In-Vitro</i> Evaluation
Pharmaceutical Nanotechnology Signal Transduction of Radiation and/or Hyperthermic Cancer Therapies
Current Signal Transduction Therapy Implications of Nanoscale Based Drug Delivery Systems in Delivery and Targeting Tubulin Binding Agent, Noscapine in Cancer Cells
Current Drug Metabolism The Relationship Between Prostate Cancer and Metformin Consumption: A Systematic Review and Meta-analysis Study
Current Pharmaceutical Design Population Diversity and its Relationship with Infectious and Tumor Diseases
Current Immunology Reviews (Discontinued) Farnesyltransferase Inhibitors: A Comprehensive Review Based on Quantitative Structural Analysis
Current Medicinal Chemistry The Role of the RhoA/rho-kinase Pathway in Pulmonary Hypertension
Current Drug Discovery Technologies Recent Progress in Stimuli-Responsive Intelligent Nano Scale Drug Delivery Systems: A Special Focus Towards pH-Sensitive Systems
Current Drug Targets Heat Shock Proteins: Therapeutic Drug Targets for Chronic Neurodegeneration?
Current Pharmaceutical Biotechnology Determinants of Smoking Cessation Attempts Among HIV-Infected Patients: Results from a Hospital-Based Prospective Cohort
Current HIV Research Toxicogenomics to Improve Comprehension of the Mechanisms Underlying Responses of In Vitro and In Vivo Systems to Nanomaterials: A Review
Current Genomics Impaired Expression and Function of Signaling Pathway Enzymes by Anthocyanins: Role on Cancer Prevention and Progression
Current Enzyme Inhibition Inflammasome Signaling in Pathogenesis of Lung Diseases
Current Pharmaceutical Design Oxidative Stress, Pro-Inflammatory Cytokines, and Antioxidants Regulate Expression Levels of MicroRNAs in Parkinson’s Disease
Current Aging Science