Abstract
A series of twenty one chalcone derivatives having indole moiety were synthesized and were evaluated against four human cancer cell lines. Indolyl chalcones 1a, 1b, 1d, 1f-1j, 2c, 2e, 2i showed good anticancer activity. Chalcones 1b and 1d were the most active and selective anticancer agents with IC50 values <1μg/ml and 1.51μg/ml, against WRL-68 cell line, respectively. Molecular mechanism was explored through in silico docking & ADMET studies.
Keywords: 1, 3-Diaryl-2-propen-1-ones, Anticancer agents, Indolyl chalcones.
Graphical Abstract
Current Topics in Medicinal Chemistry
Title:Molecular Modeling Based Synthesis and Evaluation of In vitro Anticancer Activity of Indolyl Chalcones
Volume: 15 Issue: 11
Author(s): Rashmi Gaur, Dharmendra K. Yadav, Shiv Kumar, Mahendra P. Darokar, Feroz Khan and Rajendra Singh Bhakuni
Affiliation:
Keywords: 1, 3-Diaryl-2-propen-1-ones, Anticancer agents, Indolyl chalcones.
Abstract: A series of twenty one chalcone derivatives having indole moiety were synthesized and were evaluated against four human cancer cell lines. Indolyl chalcones 1a, 1b, 1d, 1f-1j, 2c, 2e, 2i showed good anticancer activity. Chalcones 1b and 1d were the most active and selective anticancer agents with IC50 values <1μg/ml and 1.51μg/ml, against WRL-68 cell line, respectively. Molecular mechanism was explored through in silico docking & ADMET studies.
Export Options
About this article
Cite this article as:
Gaur Rashmi, Yadav K. Dharmendra, Kumar Shiv, Darokar P. Mahendra, Khan Feroz and Bhakuni Singh Rajendra, Molecular Modeling Based Synthesis and Evaluation of In vitro Anticancer Activity of Indolyl Chalcones, Current Topics in Medicinal Chemistry 2015; 15 (11) . https://dx.doi.org/10.2174/1568026615666150317222059
DOI https://dx.doi.org/10.2174/1568026615666150317222059 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- 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
- Announcements
Related Articles
-
CD147 Promotes Melanoma Progression Through Hypoxia-Induced MMP2 Activation
Current Molecular Medicine Innovative Drug Delivery Systems for the Administration of Natural Compounds
Current Bioactive Compounds Epigenetics, Depression and Antidepressant Treatment
Current Pharmaceutical Design Advances in Systemic Therapy for Gastroenteropancreatic Neuroendocrine Malignancies
Current Clinical Pharmacology Biological Properties of Yeast-based Mannoprotein for Prospective Biomedical Applications
Combinatorial Chemistry & High Throughput Screening Inflammation-Induced Thrombosis: Mechanisms, Disease Associations and Management
Current Pharmaceutical Design New Use for Old Drugs? Prospective Targets of Chloroquines in Cancer Therapy
Current Drug Targets Anti-inflammatory strategies in stroke: a potential therapeutic target
Current Vascular Pharmacology HDAC Inhibitors-New Generation of Target Specific Treatment
Mini-Reviews in Medicinal Chemistry Decoding the Inter-Relationship between Sleep Disorders and Alzheimer’s Disease Pathogenesis
CNS & Neurological Disorders - Drug Targets Honey as a Source of Dietary Antioxidants: Structures, Bioavailability and Evidence of Protective Effects Against Human Chronic Diseases
Current Medicinal Chemistry A Review on Fruit Juice Probiotication: Pomegranate
Current Nutrition & Food Science Activation of Integrin β1 Mediates the Increased Malignant Potential of Ovarian Cancer Cells Exerted by Inflammatory Cytokines
Anti-Cancer Agents in Medicinal Chemistry Editorial (Thematic Issue: Iron Chelation and Drug Resistance in Cancer and Tuberculosis)
Current Pharmaceutical Biotechnology Lifelong Endocrine Fluctuations and Related Cognitive Disorders
Current Pharmaceutical Design Renal Cell Carcinoma Cancer Stem Cells as Therapeutic Targets
Current Signal Transduction Therapy Cell Arrest and Apoptosis Induced by the Next Generation of Vanadium Based Drugs: Action Mechanism to Structure Relation and Future Perspectives
Anti-Cancer Agents in Medicinal Chemistry Meet Our Editorial Board Member
Current Medical Imaging The Nervous System as a Critical Regulator of Immune Responses Underlying Allergy
Current Pharmaceutical Design Editorial (Thematic Issue: New Mechanisms and Targets for IBD Therapy: Translational Gastroenterology Comes of Age)
Current Drug Targets