Abstract
A series of diflunisal 4-thiazolidinones were synthesized. Some selected compounds were determined at one dose towards the full panel of 60 human cancer cell lines by National Cancer Institute. 2',4'-Difluoro-4-hydroxy-N-[4-oxo-2-(thiophen-2-yl)-1,3-thiazolidin-3-yl]biphenyl- 3-carboxamide (4a) demonstrated the most marked effect on K-562 cancer cell line with 58.59 % growth inhibition at 10 μM. Compound 4a was evaluated in vitro using the MTT colorimetric method against human leukemia cell line K-562 and mouse embryonic fibroblasts cell line NIH- 3T3 at different doses for cell viability and growth inhibition. Compound 4a exhibited anticancer activity with IC50 value of 5.2 μM against K-562 cells and did not display cytotoxicity towards NIH-3T3 cells compared with diflunisal. In addition, this compound could be an interesting prototype as an antiproliferative agent.
Keywords: Annexin-V, apoptosis, diflunisal, K-562 cancer cell line, 4-Thiazolidinone.
Anti-Cancer Agents in Medicinal Chemistry
Title:Synthesis of Diflunisal Thiazolidinones as Anticancer Agents
Volume: 16 Issue: 10
Author(s): Sevil Şenkardeş, Özlem B. Özakpınar, Derya Özsavcı, Azize Şener, Özge Çevik and Ş. Güniz Küçükgüzel
Affiliation:
Keywords: Annexin-V, apoptosis, diflunisal, K-562 cancer cell line, 4-Thiazolidinone.
Abstract: A series of diflunisal 4-thiazolidinones were synthesized. Some selected compounds were determined at one dose towards the full panel of 60 human cancer cell lines by National Cancer Institute. 2',4'-Difluoro-4-hydroxy-N-[4-oxo-2-(thiophen-2-yl)-1,3-thiazolidin-3-yl]biphenyl- 3-carboxamide (4a) demonstrated the most marked effect on K-562 cancer cell line with 58.59 % growth inhibition at 10 μM. Compound 4a was evaluated in vitro using the MTT colorimetric method against human leukemia cell line K-562 and mouse embryonic fibroblasts cell line NIH- 3T3 at different doses for cell viability and growth inhibition. Compound 4a exhibited anticancer activity with IC50 value of 5.2 μM against K-562 cells and did not display cytotoxicity towards NIH-3T3 cells compared with diflunisal. In addition, this compound could be an interesting prototype as an antiproliferative agent.
Export Options
About this article
Cite this article as:
Şenkardeş Sevil, Özakpınar B. Özlem, Özsavcı Derya, Şener Azize, Çevik Özge and Küçükgüzel Güniz Ş., Synthesis of Diflunisal Thiazolidinones as Anticancer Agents, Anti-Cancer Agents in Medicinal Chemistry 2016; 16 (10) . https://dx.doi.org/10.2174/1871520615666150831125337
DOI https://dx.doi.org/10.2174/1871520615666150831125337 |
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
-
Xanthohumol: A Metabolite with Promising Anti-Neoplastic Potential
Anti-Cancer Agents in Medicinal Chemistry HIF-1 Inhibitors for Cancer Therapy: From Gene Expression to Drug Discovery
Current Pharmaceutical Design Role of Adiponectin in Cervical Cancer
Current Drug Metabolism Fe3O4 Nanoparticles Mediated Synthesis of Novel Isatin-dihydropyrimidinone Hybrid Molecules as Antioxidant and Cytotoxic Agents
Anti-Cancer Agents in Medicinal Chemistry Emerging Therapy for Diabetic Neuropathy: Cell Therapy Targeting Vessels and Nerves
Endocrine, Metabolic & Immune Disorders - Drug Targets TNF-Related Apoptosis-Inducing Ligand (TRAIL) as a Pro-Apoptotic Signal Transducer with Cancer Therapeutic Potential
Current Pharmaceutical Design Systematic Patent Review of Nanoparticles in Drug Delivery and Cancer Therapy in the Last Decade
Recent Advances in Drug Delivery and Formulation Chemical Constituents of Plants from the Genus Valeriana
Mini-Reviews in Organic Chemistry Curcumin: Not So Spicy After All
Mini-Reviews in Medicinal Chemistry Hematopoietic Growth Factors Support in the Elderly Cancer Patients Treated with Antiblastic Chemotherapy
Anti-Cancer Agents in Medicinal Chemistry Clinical Approaches Toward Tumor Angiogenesis: Past, Present and Future
Current Pharmaceutical Design Modulation of Long Non-coding RNAs by Different Classes of Secondary Metabolites from Plants: A Mini-review on Antitumor Effects
Mini-Reviews in Medicinal Chemistry Antigene and Antiproliferative Effects of Triplex-Forming Oligonucleotide (TFO) Targeted on hmgb1 Gene in Human Hepatoma Cells
Anti-Cancer Agents in Medicinal Chemistry The Influence of AIDS on the Morphometric and Immune Status of the Uterine Cervix of Autopsied Patients
Current HIV Research Designing of Novel Carbonic Anhydrase Inhibitors and Activators
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Melatonin and Hypothalamic-Pituitary-Gonadal Axis
Current Medicinal Chemistry Spatio-Temporal Expression and Functional Analysis of miR-206 in Developing Orofacial Tissue
MicroRNA Spirooxindoles as Potential Pharmacophores
Mini-Reviews in Medicinal Chemistry Nucleic Acid-Based Aptamers: Applications, Development and Clinical Trials
Current Medicinal Chemistry Phytochemical Characterization of Prickly Pear (Opuntia spp.) and of its Nutritional and Functional Properties: A Review
Current Nutrition & Food Science