Abstract
A new series of N-substituted 2-butyl-5-chloro-3H-imidazole-4-carbaldehyde derivatives were synthesized by using the different bioactive heteroaralkyl halides with 2-butyl-4-chloro-1H-imidazole-5-carbaldehyde in presence of powdered potassium carbonate in DMF medium. These compounds were screened for their antitumor activity. Our results show that treatment of imidazole derivatives inhibit proliferation EAT cells, decreases the ascites volume and increases the survivability of the animals in vivo. These compounds also inhibited the cellular proliferation of HUVEC cells in vitro by MTT assay. Further, these compounds could induce apoptosis, which is evident by the nuclear condensation of imidazole derivatives treated EAT cells in vivo by the cytological analysis. We have identified that pyrrolidine substituted imidazole derivative as potent anti-tumor compound. These inhibitors could represent as promising candidates for anticancer therapies, where the formation of peritoneal malignant ascites is a major cause of morbidity and mortality.
Keywords: Antitumor activity, HUVEC, imidazole derivative, EAT cells
Medicinal Chemistry
Title: N-Substituted-2-butyl-5-chloro-3H-imidazole-4-carbaldehyde Derivatives as Anti-tumor Agents Against Ehrlich Ascites tumor Cells In Vivo
Volume: 3 Issue: 3
Author(s): C. Anil Kumar, S. Nanjunda Swamy, S. L. Gaonkar, Basappa, Bharathi P. Salimath and Kanchugarakoppal S. Rangappa
Affiliation:
Keywords: Antitumor activity, HUVEC, imidazole derivative, EAT cells
Abstract: A new series of N-substituted 2-butyl-5-chloro-3H-imidazole-4-carbaldehyde derivatives were synthesized by using the different bioactive heteroaralkyl halides with 2-butyl-4-chloro-1H-imidazole-5-carbaldehyde in presence of powdered potassium carbonate in DMF medium. These compounds were screened for their antitumor activity. Our results show that treatment of imidazole derivatives inhibit proliferation EAT cells, decreases the ascites volume and increases the survivability of the animals in vivo. These compounds also inhibited the cellular proliferation of HUVEC cells in vitro by MTT assay. Further, these compounds could induce apoptosis, which is evident by the nuclear condensation of imidazole derivatives treated EAT cells in vivo by the cytological analysis. We have identified that pyrrolidine substituted imidazole derivative as potent anti-tumor compound. These inhibitors could represent as promising candidates for anticancer therapies, where the formation of peritoneal malignant ascites is a major cause of morbidity and mortality.
Export Options
About this article
Cite this article as:
Anil Kumar C., Nanjunda Swamy S., Gaonkar L. S., Basappa , Salimath P. Bharathi and Rangappa S. Kanchugarakoppal, N-Substituted-2-butyl-5-chloro-3H-imidazole-4-carbaldehyde Derivatives as Anti-tumor Agents Against Ehrlich Ascites tumor Cells In Vivo, Medicinal Chemistry 2007; 3 (3) . https://dx.doi.org/10.2174/157340607780620699
DOI https://dx.doi.org/10.2174/157340607780620699 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
![](/images/wayfinder.jpg)
- 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
-
Effect of Selenium-Saturated Bovine Lactoferrin (Se-bLF) on Antioxidant Enzyme Activities in Human Gut Epithelial Cells Under Oxidative Stress
Anti-Cancer Agents in Medicinal Chemistry MAVS: A New Weapon in the Fight Against Viral Infections
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Microbubble-Assisted p53, RB, and p130 Gene Transfer in Combination with Radiation Therapy in Prostate Cancer
Current Gene Therapy Increased Induction of Apoptosis in ESCC (Esophageal Squamous-Cell Carcinoma) by Betula pendula Roth Stem Cell Extract Containing Triterpenoids Compared to Doxorubicin
Anti-Cancer Agents in Medicinal Chemistry Therapies of Hematological Malignancies: An Overview of the Potential Targets and Their Inhibitors
Current Chemical Biology Lipid Nanoparticles as a Skin Wound Healing Drug Delivery System: Discoveries and Advances
Current Pharmaceutical Design Survey of Functional Activities of Alpha-fetoprotein Derived Growth Inhibitory Peptides: Review and Prospects
Current Protein & Peptide Science Nanomedicine against Alzheimer’s and Parkinson’s Disease
Current Pharmaceutical Design Mitochondrial and Nuclear Genes of Mitochondrial Components in Cancer
Current Genomics Vitamin D, Pit-1, GH, and PRL: Possible Roles in Breast Cancer Development
Current Medicinal Chemistry Clinical Outcomes of the Transplantation of Stem Cells from Various Human Tissue Sources in the Management of Liver Cirrhosis: A Systematic Review and Meta-Analysis
Current Stem Cell Research & Therapy Drug Discovery and Protein Tyrosine Phosphatases
Current Medicinal Chemistry A Hypothesis for Regenerative Therapy for Neuronal Disease: Stem Cells within Artificial Niche
Current Signal Transduction Therapy Polyunsaturated Fatty Acids in Pregnancy and Metabolic Syndrome: A Review
Current Pharmaceutical Biotechnology Dynamic Contrast-Enhanced Magnetic Resonance Imaging for Differentiating Between Primary Tumor, Metastatic Node and Normal Tissue in Head and Neck Cancer
Current Medical Imaging Therapeutic Targets for Metastatic Prostate Cancer
Current Drug Targets Lymphocyte Biomarkers of Clinical Responses to Adoptive Immunotherapy of Malignant Melanoma
Current Cancer Therapy Reviews Editorial: [Exciting Discoveries About New p53 Target Genes, Cancer Drugs and Diagnostic Tools, and Mechanisms of Various Human Diseases]
Current Molecular Medicine Main Anti-tumor Angiogenesis Agents Isolated From Chinese Herbal Medicines
Mini-Reviews in Medicinal Chemistry Astrocytes: Adhesion Molecules and Immunomodulation
Current Drug Targets