Abstract
Objective/Method: A group of 4-benzoyl-1-dichlorobenzoylthiosemicarbazides endowed with antibacterial activity was evaluated for its cytotoxic properties against breast cancer cells (MCF-7, MDA-MB-231) and head and neck squamous cell carcinomas (FaDu, SCC-25). Cytotoxicity of the investigated compounds was measured using MTT and [3H]-thymidine incorporation bioassays.
Result: 1-(2,3-Dichlorobenzoyl)-4-(2-methylbenzoyl)thiosemicarbazide (TA-4), 1-(2,4-dichlorobenzoyl)- 4-(2-methylbenzoyl)thiosemicarbazide (TA-18), and 1-(2,4-dichlorobenzoyl)-4-(4-nitrolbenzoyl)- thiosemicarbazide (TA-20) were found to possess anticancer activity equipotent or even stronger than that of reference drug – etoposide. In order to clarify the molecular mode of action of the mentioned compounds, the relaxation assay kit for human DNA topoisomerase II was used. It turned out that reduction of viability of cancer cells was a result of inhibition of human DNA topoII. Molecular docking studies proved that 4-benzoyl-1-dichlorobenzoylthiosemicarbazides strongly interact with DNAdependent subunit of that enzyme.
Keywords: Human DNA topoisomerase, MTT assay, [3H]-thymidine incorporation assay, breast cancer cells head and neck squamous cell carcinomas (HNSCC).
Anti-Cancer Agents in Medicinal Chemistry
Title:Dual Antibacterial and Anticancer Activity of 4-Benzoyl-1-dichlorobenzoylthiosemicarbazide Derivatives
Volume: 18 Issue: 4
Author(s): Barbara Kapron, Robert Czarnomysy, Agata Paneth, Monika Wujec, Krzysztof Bielawski, Anna Bielawska, Lukasz Swiatek, Barbara Rajtar, Malgorzata Polz-Dacewicz and Tomasz Plech*
Affiliation:
- Department of Pharmacology, Medical University of Lublin, Chodzki 4a, 20-093 Lublin,Poland
Keywords: Human DNA topoisomerase, MTT assay, [3H]-thymidine incorporation assay, breast cancer cells head and neck squamous cell carcinomas (HNSCC).
Abstract: Objective/Method: A group of 4-benzoyl-1-dichlorobenzoylthiosemicarbazides endowed with antibacterial activity was evaluated for its cytotoxic properties against breast cancer cells (MCF-7, MDA-MB-231) and head and neck squamous cell carcinomas (FaDu, SCC-25). Cytotoxicity of the investigated compounds was measured using MTT and [3H]-thymidine incorporation bioassays.
Result: 1-(2,3-Dichlorobenzoyl)-4-(2-methylbenzoyl)thiosemicarbazide (TA-4), 1-(2,4-dichlorobenzoyl)- 4-(2-methylbenzoyl)thiosemicarbazide (TA-18), and 1-(2,4-dichlorobenzoyl)-4-(4-nitrolbenzoyl)- thiosemicarbazide (TA-20) were found to possess anticancer activity equipotent or even stronger than that of reference drug – etoposide. In order to clarify the molecular mode of action of the mentioned compounds, the relaxation assay kit for human DNA topoisomerase II was used. It turned out that reduction of viability of cancer cells was a result of inhibition of human DNA topoII. Molecular docking studies proved that 4-benzoyl-1-dichlorobenzoylthiosemicarbazides strongly interact with DNAdependent subunit of that enzyme.
Export Options
About this article
Cite this article as:
Kapron Barbara , Czarnomysy Robert , Paneth Agata , Wujec Monika , Bielawski Krzysztof , Bielawska Anna , Swiatek Lukasz, Rajtar Barbara , Polz-Dacewicz Malgorzata and Plech Tomasz *, Dual Antibacterial and Anticancer Activity of 4-Benzoyl-1-dichlorobenzoylthiosemicarbazide Derivatives, Anti-Cancer Agents in Medicinal Chemistry 2018; 18 (4) . https://dx.doi.org/10.2174/1871520617666171023142958
DOI https://dx.doi.org/10.2174/1871520617666171023142958 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...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/Testis Antigens Trigger Epithelial-Mesenchymal Transition and Genesis of Cancer Stem-Like Cells
Current Pharmaceutical Design Integrins: A Method of Early Intervention in the Treatment of Colorectal Liver Metastases
Current Pharmaceutical Design Targeting Receptor Tyrosine Kinases Using Monoclonal Antibodies: The Most Specific Tools for Targeted-Based Cancer Therapy
Current Drug Targets Potential Mechanisms for Increased HIV-1 Transmission Across the Endocervical Epithelium During C. trachomatis Infection
Current HIV Research Allelic Imbalances of the egfr Gene as Key Events in Breast Cancer Progression – the Concept of Committed Progenitor Cells
Current Cancer Drug Targets Serum Carboxypeptidase N1 Serves as a Potential Biomarker Complementing CA15-3 for Breast Cancer
Anti-Cancer Agents in Medicinal Chemistry The Use of L-Glucose in Cancer Diagnosis: Results from In Vitro and In Vivo Studies
Current Medicinal Chemistry Neuroblastoma and Stem Cell Therapy: An Updated Review
CNS & Neurological Disorders - Drug Targets MicroRNAs-based Therapy: A Novel and Promising Strategy for Cancer Treatment
MicroRNA HSF1, A Versatile Factor in Tumorogenesis
Current Molecular Medicine Polymeric Nanoparticles to Combat Squamous Cell Carcinomas in Patients with Dystrophic Epidermolysis Bullosa
Recent Patents on Nanomedicine Receptor Tyrosine Kinases are Signaling Intermediates of G Protein- Coupled Receptors
Current Pharmaceutical Design Clinical and <i>In Silico</i> Outcomes of the Expression of miR-130a-5p and miR-615-3p in Tumor Compared with Non-Tumor Adjacent Tissues of Patients with BC
Anti-Cancer Agents in Medicinal Chemistry Delivery Methods of Camptothecin and Its Hydrosoluble Analogue Irinotecan for Treatment of Colorectal Cancer
Current Drug Delivery Histotype in Non-Small Cell Lung Cancer Therapy and Staging: The Emerging Role of an Old and Underrated Factor
Current Respiratory Medicine Reviews Targeting IAPs as An Approach to Anti-Cancer Therapy
Current Topics in Medicinal Chemistry Oxidative Phosphorylation as a Target to Arrest Malignant Neoplasias
Current Medicinal Chemistry Selenium Compounds Biotransformed by Mushrooms: Not Only Dietary Sources, But Also Toxicity Mediators
Current Nutrition & Food Science Dual Roles of Sulforaphane in Cancer Treatment
Anti-Cancer Agents in Medicinal Chemistry Green Synthesis of Silver Nanocomposites of Nigella sativa Seeds Extract for Hepatocellular Carcinoma
Current Nanomaterials