Abstract
4,6-diarylpyrimidones as constrained chalcone analogues have been synthesised in the present study. The synthesised compounds were evaluated against a panel of human cancer cell lines. Striking selectivity was displayed by the compounds against MiaPaCa (Pancreatic) cell lines while PC-3 (prostate) and A-549 (lung) cell lines were almost resistant to the exposure of the test compounds. Compound SK – 25 exhibited remarkable cytotoxicity against MiaPaca-2 cell line with an IC50 value of 1.95 µM and was found to induce apoptosis evidenced through phase contrast microscopy, DAPI staining and mitochondrial membrane potential loss. The cell phase distribution studies indicated that the apoptotic population increased from 1.79% in control sample to 30.33 % in sample treated with 20 µM compound SK-25.
Keywords: Apoptosis, cell cycle, chalcone, contrained, cytotoxic, pyrimidones.
Anti-Cancer Agents in Medicinal Chemistry
Title:4,6-diaryl Pyrimidones as Constrained Chalcone Analogues: Design, Synthesis and Evaluation as Antiproliferative Agents
Volume: 15 Issue: 6
Author(s): Dinesh Kumar, Kunal Nepali, PMS Bedi, Suresh Kumar, Fayaz Malik and Subheet Jain
Affiliation:
Keywords: Apoptosis, cell cycle, chalcone, contrained, cytotoxic, pyrimidones.
Abstract: 4,6-diarylpyrimidones as constrained chalcone analogues have been synthesised in the present study. The synthesised compounds were evaluated against a panel of human cancer cell lines. Striking selectivity was displayed by the compounds against MiaPaCa (Pancreatic) cell lines while PC-3 (prostate) and A-549 (lung) cell lines were almost resistant to the exposure of the test compounds. Compound SK – 25 exhibited remarkable cytotoxicity against MiaPaca-2 cell line with an IC50 value of 1.95 µM and was found to induce apoptosis evidenced through phase contrast microscopy, DAPI staining and mitochondrial membrane potential loss. The cell phase distribution studies indicated that the apoptotic population increased from 1.79% in control sample to 30.33 % in sample treated with 20 µM compound SK-25.
Export Options
About this article
Cite this article as:
Kumar Dinesh, Nepali Kunal, Bedi PMS, Kumar Suresh, Malik Fayaz and Jain Subheet, 4,6-diaryl Pyrimidones as Constrained Chalcone Analogues: Design, Synthesis and Evaluation as Antiproliferative Agents, Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (6) . https://dx.doi.org/10.2174/1871520615666150318101436
DOI https://dx.doi.org/10.2174/1871520615666150318101436 |
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
-
Application of MALDI/SELDI Mass Spectrometry to Cancer Biomarker Discovery and Validation
Current Proteomics Tumor Markers: The Potential of “Omics” Approach
Current Molecular Medicine Bortezomib in the Treatment of Cancer
Recent Patents on Anti-Cancer Drug Discovery Structure Based Design, Synthesis, and Evaluation of Potential Inhibitors of Steroid Sulfatase
Current Topics in Medicinal Chemistry Mammaglobin-Based Strategies for Treatment of Breast Cancer
Current Cancer Drug Targets Targeting the Endocannabinoid System for the Treatment of Cancer – A Practical View
Current Topics in Medicinal Chemistry Detection of Predictive Markers for Therapeutic Stratification of Salivary Glands Tumors
Current Drug Targets Synthetic Approaches to Functionalized Lipids for Protein Monolayer Crystallizations
Current Organic Chemistry Hematological Targets of Radiation Damage
Current Drug Targets Design, Synthesis and Antiproliferative Activity of 2-Acetamidothiazole-5- carboxamide Derivatives
Medicinal Chemistry New Functions of the Inositol Polyphosphate 5-Phosphatases in Cancer
Current Pharmaceutical Design Oxaliplapin and Capecitabine (XELOX) Based Chemotherapy in the Treatment of Metastatic Colorectal Cancer: The Right Choice in Elderly Patients
Anti-Cancer Agents in Medicinal Chemistry H3K4 Methylation Status and Lysine Specific Methyltransferase KMT2C Expression Correlate with Prognosis in Lung Adenocarcinoma
Current Molecular Pharmacology Regulation of ABC Transporter Function Via Phosphorylation by Protein Kinases
Current Pharmaceutical Biotechnology ADAM Proteins- Therapeutic Potential in Cancer
Current Cancer Drug Targets Genomic and Cellular Pathology of Lung Cancer
Current Respiratory Medicine Reviews Myokines in Myogenesis and Health
Recent Patents on Biotechnology In vivo Radiosensitization of Human Glioma U87 Cells Induced by Upregulated Expression of DUSP-2 after Treatment with Curcumin
Current Signal Transduction Therapy A Better Platinum-Based Anticancer Drug Yet to Come?
Anti-Cancer Agents in Medicinal Chemistry The Ubiquitin-Proteasome System and Proteasome Inhibitors in Central Nervous System Diseases
Cardiovascular & Hematological Disorders-Drug Targets