Abstract
Background: Triazine ring is a prominent structural motif found in some azanucleosides whose efficiency improved many times in the research area of antitumor agents.
Objective: In this study, we have designed and synthesized novel 2-[(5,6-diphenyl-1,2,4-triazin-3-yl)thio]-N-(6- substituted benzo/(thiazol)-2-yl)acetamide (2a-d, 3a-f) derivatives using 1,2,4-triazine core along with two important heterocyles, thiazole and benzothiazole rings.
Method: The acquired ten final compounds were screened to investigate their antitumor activity against lung adenocarcinoma cell line, A549 and mouse fibroblast cell line, NIH/3T3. Five compounds with higher antiproliferative activity have been further studied to evaluate whether the cell death due to necrosis or apoptosis using flow cytometry.
Results and Conclusion: Compound 3b bearing 6-methylbenzothiazole moiety has been established as the most active antitumor compound with a selective profile and higher apoptotic cell level. All final componds were also screened against acetylcholine/butyrylcholinesterase enzymes to state their anticholinesterase activity.
Keywords: Triazine, thiazole, benzothiazole, antiproliferative activity, lung cancer, apoptosis.
Anti-Cancer Agents in Medicinal Chemistry
Title:Biological Activity Evaluation of Novel 1,2,4-Triazine Derivatives Containing Thiazole/Benzothiazole Rings
Volume: 17 Issue: 13
Author(s): Leyla Yurttas*, Gulsen Akalin Ciftci, Halide Edip Temel, Begum Nurpelin Saglik, Bahar Demir and Serkan Levent
Affiliation:
- Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Anadolu University, 26470 Eskisehir,Turkey
Keywords: Triazine, thiazole, benzothiazole, antiproliferative activity, lung cancer, apoptosis.
Abstract: Background: Triazine ring is a prominent structural motif found in some azanucleosides whose efficiency improved many times in the research area of antitumor agents.
Objective: In this study, we have designed and synthesized novel 2-[(5,6-diphenyl-1,2,4-triazin-3-yl)thio]-N-(6- substituted benzo/(thiazol)-2-yl)acetamide (2a-d, 3a-f) derivatives using 1,2,4-triazine core along with two important heterocyles, thiazole and benzothiazole rings.
Method: The acquired ten final compounds were screened to investigate their antitumor activity against lung adenocarcinoma cell line, A549 and mouse fibroblast cell line, NIH/3T3. Five compounds with higher antiproliferative activity have been further studied to evaluate whether the cell death due to necrosis or apoptosis using flow cytometry.
Results and Conclusion: Compound 3b bearing 6-methylbenzothiazole moiety has been established as the most active antitumor compound with a selective profile and higher apoptotic cell level. All final componds were also screened against acetylcholine/butyrylcholinesterase enzymes to state their anticholinesterase activity.
Export Options
About this article
Cite this article as:
Yurttas Leyla*, Ciftci Akalin Gulsen, Temel Edip Halide , Saglik Nurpelin Begum, Demir Bahar and Levent Serkan , Biological Activity Evaluation of Novel 1,2,4-Triazine Derivatives Containing Thiazole/Benzothiazole Rings, Anti-Cancer Agents in Medicinal Chemistry 2017; 17 (13) . https://dx.doi.org/10.2174/1871520617666170327151031
DOI https://dx.doi.org/10.2174/1871520617666170327151031 |
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
-
The Role of Shcbp1 in Signaling and Disease
Current Cancer Drug Targets Preventive and Protective Roles of Dietary Nrf2 Activators Against Central Nervous System Diseases
CNS & Neurological Disorders - Drug Targets T11TS/SLFA-3 Differentially Regulate the Population of Microglia and Brain Infiltrating Lymphocytes to Reduce Glioma by Modulating Intrinsic Bcl-2 Expression rather than p53
Central Nervous System Agents in Medicinal Chemistry Melittin: A Natural Peptide with Expanded Therapeutic Applications
The Natural Products Journal Bacteria and Bacterial Toxins as Therapeutic Agents for Solid Tumors
Current Cancer Drug Targets Advances in the Researches on the Biological Activities and Inhibitors of Phosphatidylinositol 3-kinase
Anti-Cancer Agents in Medicinal Chemistry The Association between Tumor-associated Macrophages and Glioblastoma: A Potential Target for Therapy
Current Pharmaceutical Design Proteomic Analysis of Glioma Chemoresistance
Current Neuropharmacology Drug Metabolism and Pharmacokinetics of Dammarane Triterpenoids
Current Drug Metabolism Genetic and Epigenetic Studies for Determining Molecular Targets of Natural Product Anticancer Agents
Current Cancer Drug Targets Differentiation-Inducing Therapy for Solid Tumors
Current Pharmaceutical Design Biologically Active Peptides Interacting with the G Protein-Coupled Formylpeptide Receptors
Protein & Peptide Letters Role of Calcium, Vitamin D, and the Extrarenal Vitamin D Hydroxylases in Carcinogenesis
Anti-Cancer Agents in Medicinal Chemistry Meet Our Editorial Board Member
Current Medical Imaging Herpes Simplex Virus Vectors for Gene Delivery to a Variety of Different Cell Types
Current Gene Therapy Biological Activity and Physicochemical Properties of Dipeptidyl Nitrile Derivatives Against Pancreatic Ductal Adenocarcinoma Cells
Anti-Cancer Agents in Medicinal Chemistry Post-Translational Modifications of PTEN and their Potential Therapeutic Implications
Current Cancer Drug Targets Interferon Therapy for Malignant Solid Tumors
Current Drug Therapy A Fatal Case of Acute Interstitial Pneumonia (AIP) in a Woman Affected by Glioblastoma
Current Drug Safety Nanoparticle Systems Modulating Myeloid-Derived Suppressor Cells for Cancer Immunotherapy
Current Topics in Medicinal Chemistry