Abstract
α-N-Heterocyclic thiosemicarbazones, (N)-TSCs, are potent inhibitors of ribonucleotide reductase (RR). This enzyme plays a critical role in DNA synthesis and repair, and is a well-recognized target for cancer chemotherapeutic agents. In this review the structural features of (N)-TSCs, required for maximum antitumour activity have been explored. Special attention is given to the mechanisms of action and structure-activity relationships.
Keywords: α-N-heterocyclic thiosemicarbazone, bis(thiosemicarbazone), ribonucleotide reductase inhibitors, antitumour agents, metal complexes, structure-activity relationships
Mini-Reviews in Medicinal Chemistry
Title: α-N-Heterocyclic Thiosemicarbazone Derivatives as Potential Antitumor Agents: A Structure-Activity Relationships Approach
Volume: 9 Issue: 12
Author(s): Ana I. Matesanz and Pilar Souza
Affiliation:
Keywords: α-N-heterocyclic thiosemicarbazone, bis(thiosemicarbazone), ribonucleotide reductase inhibitors, antitumour agents, metal complexes, structure-activity relationships
Abstract: α-N-Heterocyclic thiosemicarbazones, (N)-TSCs, are potent inhibitors of ribonucleotide reductase (RR). This enzyme plays a critical role in DNA synthesis and repair, and is a well-recognized target for cancer chemotherapeutic agents. In this review the structural features of (N)-TSCs, required for maximum antitumour activity have been explored. Special attention is given to the mechanisms of action and structure-activity relationships.
Export Options
About this article
Cite this article as:
Matesanz I. Ana and Souza Pilar, α-N-Heterocyclic Thiosemicarbazone Derivatives as Potential Antitumor Agents: A Structure-Activity Relationships Approach, Mini-Reviews in Medicinal Chemistry 2009; 9 (12) . https://dx.doi.org/10.2174/138955709789957422
DOI https://dx.doi.org/10.2174/138955709789957422 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...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
-
Nitrogen-Containing Heterocycles as Anticancer Agents: An Overview
Anti-Cancer Agents in Medicinal Chemistry Inhibition of Apoptosis in Pediatric Cancer by Survivin
Current Pediatric Reviews Editorial (Thematic Issue: Special Thematic Issue: Crossreactivity in Cancer and Autoimmunity)
Anti-Cancer Agents in Medicinal Chemistry Cyclin-Dependent Kinase-2 as a Target for Cancer Therapy: Progress in the Development of CDK2 Inhibitors as Anti-Cancer Agents
Current Medicinal Chemistry [6]-gingerol as a Cancer Chemopreventive Agent: A Review of Its Activity on Different Steps of the Metastatic Process
Mini-Reviews in Medicinal Chemistry Mucin-based Targeted Pancreatic Cancer Therapy
Current Pharmaceutical Design Recent Advances and Developments in Treatment Strategies Against Pancreatic Cancer
Current Clinical Pharmacology Expression, Purification, Crystallization and Preliminary X-Ray Analysis of Human Spindlin1, an Ovarian Cancer-Related Protein
Protein & Peptide Letters The Pro-Survival Function of Akt Kinase can be Overridden or Altered to Contribute to Induction of Apoptosis
Current Cancer Drug Targets Imaging of HER-2 Overexpression in Tumors for Guiding Therapy
Current Pharmaceutical Design Identification of Prognostic Biomarkers in Papillary Thyroid Cancer and Developing Non-Invasive Diagnostic Models Through Integrated Bioinformatics Analysis
MicroRNA Potentials and Challenges of Active Targeting at the Tumor Cells by Engineered Polymeric Nanoparticles
Current Pharmaceutical Biotechnology Intrinsic Disorder in Male Sex Determination: Disorderedness of Proteins from the Sry Transcriptional Network
Current Protein & Peptide Science Potential Use of Vanadium Compounds in Therapeutics
Current Medicinal Chemistry Cellular Responses to 24R,25-dihydroxyvitamin D3 in Bone and Cartilage
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Comprehensive Review of Cancer Chemopreventive Agents Evaluated in Experimental Carcinogenesis Models and Clinical Trials
Current Medicinal Chemistry NAD<sup>+</sup>/NADH Metabolism and NAD<sup>+</sup>-Dependent Enzymes in Cell Death and Ischemic Brain Injury: Current Advances and Therapeutic Implications
Current Medicinal Chemistry Mining the Adenovirus "Virome" for Systemic Oncolytics
Current Pharmaceutical Biotechnology Comparison of the Structure and Biological Activities of Wild-type and Mutant Liver-targeting Peptide Modified Recombinant Human Endostatin (rES-CSP) in Human Hepatocellular Carcinoma HepG2 Cells
Protein & Peptide Letters Role of Cervical Cancer Radiotherapy in the Expression of EGFR and p53 Gene
Current Proteomics