Abstract
A series of 1,3,6-triphenylpyrazolo[3,4-b]pyridin-4-one derivatives was designed, synthesized and evaluated for cytotoxic activity in A375 human melanoma and human erythroleukemia (HEL) cells. The new pyrazolopyridones displayed comparable activities to the antitumor compound etoposide. The inhibitory effect of compounds 17, 18, 27 and 32 against topoisomerase II-mediated cleavage activities was measured finding good correlation with the results obtained from MTS assay. Docking studies into bacterial topoisomerase II (DNA Gyrase), topoisomerase IIα and topoisomerase IIβ binding sites in the DNA binding interface were performed.
Keywords: Pyrazolo[3, 4-b]pyridine, etoposide, topoisomerase, docking studies.
Medicinal Chemistry
Title:Synthesis and Biological Evaluation of Pyrazolo[3,4-b]pyridin-4-ones as a New Class of Topoisomerase II Inhibitors
Volume: 11 Issue: 4
Author(s): Mojgan Aghazadeh Tabrizi, Pier Giovanni Baraldi, Stefania Baraldi, Filippo Prencipe, Delia Preti, Giulia Saponaro, Romeo Romagnoli, Stefania Gessi, Stefania Merighi, Angela Stefanelli, Debora Fazzi, Pier Andrea Borea, Rodolfo Couto Maia, Nelilma C. Romeiro, Carlos A. M. Fraga and Eliezer J. Barreiro
Affiliation:
Keywords: Pyrazolo[3, 4-b]pyridine, etoposide, topoisomerase, docking studies.
Abstract: A series of 1,3,6-triphenylpyrazolo[3,4-b]pyridin-4-one derivatives was designed, synthesized and evaluated for cytotoxic activity in A375 human melanoma and human erythroleukemia (HEL) cells. The new pyrazolopyridones displayed comparable activities to the antitumor compound etoposide. The inhibitory effect of compounds 17, 18, 27 and 32 against topoisomerase II-mediated cleavage activities was measured finding good correlation with the results obtained from MTS assay. Docking studies into bacterial topoisomerase II (DNA Gyrase), topoisomerase IIα and topoisomerase IIβ binding sites in the DNA binding interface were performed.
Export Options
About this article
Cite this article as:
Tabrizi Aghazadeh Mojgan, Baraldi Giovanni Pier, Baraldi Stefania, Prencipe Filippo, Preti Delia, Saponaro Giulia, Romagnoli Romeo, Gessi Stefania, Merighi Stefania, Stefanelli Angela, Fazzi Debora, Borea Andrea Pier, Maia Couto Rodolfo, Romeiro C. Nelilma, Fraga A. M. Carlos and Barreiro J. Eliezer, Synthesis and Biological Evaluation of Pyrazolo[3,4-b]pyridin-4-ones as a New Class of Topoisomerase II Inhibitors, Medicinal Chemistry 2015; 11 (4) . https://dx.doi.org/10.2174/1573406411666141210141317
DOI https://dx.doi.org/10.2174/1573406411666141210141317 |
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
-
Cancer Chemoprevention with Green Tea Catechins: From Bench to Bed
Current Drug Targets Metabolic Remodeling Induced by Adipocytes: A New Achilles' Heel in Invasive Breast Cancer?
Current Medicinal Chemistry Human Cancer Cell Line Based Approach of 1,3,4-thiadiazole and its Fused Ring: A Comprehensive Review
Anti-Cancer Agents in Medicinal Chemistry Long Non-coding RNA HOTAIR Promotes Parkinson's Disease Induced by MPTP Through up-regulating the Expression of LRRK2
Current Neurovascular Research Nanoparticles: A Neurotoxicological Perspective
CNS & Neurological Disorders - Drug Targets Smart Polymers and Their Role in Drug Delivery: A Review
Current Drug Therapy Vascular Endothelial Cell Growth Factor (VEGF), An Emerging Target for Cancer Chemotherapy
Current Medicinal Chemistry - Anti-Cancer Agents Immunobiologic Agents in Dermatology
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry New Insights into Redox-Modulated Cell Signaling
Current Pharmaceutical Design Perspectives of Benzimidazole Derivatives as Anticancer Agents in the New Era
Anti-Cancer Agents in Medicinal Chemistry Active Targeting Strategies for Anticancer Drug Nanocarriers
Current Drug Delivery Synthetic Lethal Interactions in Cancer Therapy
Current Cancer Drug Targets Scutellarin Suppresses RPMI7951 Melanoma Cell Proliferation by Targeting TOPK
Anti-Cancer Agents in Medicinal Chemistry Is There Anybody in There? On The Mechanisms of Wall Crossing of Cell Penetrating Peptides
Current Protein & Peptide Science Role of CD73 in Disease: Promising Prognostic Indicator and Therapeutic Target
Current Medicinal Chemistry Genistein as a Potential Anticancer Agent Against Head and Neck Squamous Cell Carcinoma
Current Topics in Medicinal Chemistry P-Glycoprotein and Breast Cancer Resistance Protein Affect Disposition of Tandutinib, A Tyrosine Kinase Inhibitor
Drug Metabolism Letters Advancement of Mechanisms of Coxsackie Virus B3-Induced Myocarditis Pathogenesis and the Potential Therapeutic Targets
Current Drug Targets Application of Solvent Influenced Fluorescence-quenching and Enhancement to Develop a Highly Sensitive HPLC Methodology for Analysis of Resveratrol-PEG Conjugates
Current Pharmaceutical Analysis Fragment-Based Drug Discovery and Molecular Docking in Drug Design
Current Pharmaceutical Biotechnology