Abstract
Background: Now-a-days, the model of “hybrid drugs” has acquired recognition in medicine due to their significant role in the treatment of different health problems.
Methods: We have synthesized new series of isoxazole-chalcone conjugates (14a-m) by the Claisen-Schmidt condensation of suitable substituted acetophenones with isoxazole aldehydes (12a-d). In vitro cytotoxic activity of the synthesized compounds was studied against four different selected human cancer cell lines by using sulforhodamine B (SRB) method.
Results: The adopted scheme resulted in good yields of new series of isoxazole-chalcone conjugates (14a-m). Potent cytotoxic activity was observed for compounds -14a, 14b, 14e, 14i, 14j and 14k against prostate DU-145 cancer cell line.
Conclusion: The observed potent cytotoxic activities were due to the presence of 3,4,5- trimethoxyphenyl group.
Keywords: l-(3, 4, 5-trimethoxyphenyl)ethanone, isoxazole-chalcone, hybrid molecules, antiproliferative activity, claisenschmidt condensation, cytotoxic activities.
Letters in Drug Design & Discovery
Title:Novel Hybrid Molecules of Isoxazole Chalcone Derivatives: Synthesis and Study of in vitro Cytotoxic Activities
Volume: 15 Issue: 6
Author(s): Arunkumar Thiriveedhi*, Ratnakaram Venkata Nadh, Navuluri Srinivasu and Kishore Kaushal
Affiliation:
- Division of Chemistry, Department of Science and Humanities, Vignan's Foundation for Science Technology and Research University, Guntur-522213,India
Keywords: l-(3, 4, 5-trimethoxyphenyl)ethanone, isoxazole-chalcone, hybrid molecules, antiproliferative activity, claisenschmidt condensation, cytotoxic activities.
Abstract: Background: Now-a-days, the model of “hybrid drugs” has acquired recognition in medicine due to their significant role in the treatment of different health problems.
Methods: We have synthesized new series of isoxazole-chalcone conjugates (14a-m) by the Claisen-Schmidt condensation of suitable substituted acetophenones with isoxazole aldehydes (12a-d). In vitro cytotoxic activity of the synthesized compounds was studied against four different selected human cancer cell lines by using sulforhodamine B (SRB) method.
Results: The adopted scheme resulted in good yields of new series of isoxazole-chalcone conjugates (14a-m). Potent cytotoxic activity was observed for compounds -14a, 14b, 14e, 14i, 14j and 14k against prostate DU-145 cancer cell line.
Conclusion: The observed potent cytotoxic activities were due to the presence of 3,4,5- trimethoxyphenyl group.
Export Options
About this article
Cite this article as:
Thiriveedhi Arunkumar *, Venkata Nadh Ratnakaram , Srinivasu Navuluri and Kaushal Kishore , Novel Hybrid Molecules of Isoxazole Chalcone Derivatives: Synthesis and Study of in vitro Cytotoxic Activities, Letters in Drug Design & Discovery 2018; 15 (6) . https://dx.doi.org/10.2174/1570180814666170914121740
DOI https://dx.doi.org/10.2174/1570180814666170914121740 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
-
Adenovirus-based Immunotherapy for Prostate Cancer
Current Cancer Therapy Reviews Omacetaxine as an Anticancer Therapeutic: What is Old is New Again
Current Pharmaceutical Design Cisplatin Properties in a Nanobiotechnological Approach to Cancer: A Mini-Review
Current Cancer Drug Targets Quinazolines as Apoptosis Inducers and Inhibitors: A Review of Patent Literature
Recent Patents on Anti-Cancer Drug Discovery HAMPT, A Novel Quadruple Drug Combination Designed for Cancer Metastatic Chemoprevention: From Hypothesis to Proof-of-concept
Current Cancer Drug Targets Lipid Nanoparticles for the Delivery of Biopharmaceuticals
Current Pharmaceutical Biotechnology The Pharmacogenomics “Side-effect” of TP53/EGFR in Non-small Cell Lung Cancer Accompanied with Atorvastatin Therapy: A Functional Network Analysis
Anti-Cancer Agents in Medicinal Chemistry Urine-derived Stem Cells, A New Source of Seed Cells for Tissue Engineering
Current Stem Cell Research & Therapy Possible Consequences of Blocking Transient Receptor Potential Vanilloid 1
Current Pharmaceutical Biotechnology Cytokine and Immune System Abnormalities in Fibromyalgia and Other Central Sensitivity Syndromes
Current Rheumatology Reviews Antibodies Against Muscarinic Receptors in Breast Cancer: Agonizing Tumor Growth
Current Immunology Reviews (Discontinued) Perspectives of New Therapies for Endometriosis
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Current Strategies to Target the Anti-Apoptotic Bcl-2 Protein in Cancer Cells
Current Medicinal Chemistry Gas1 is a Pleiotropic Regulator of Cellular Functions: from Embryonic Development to Molecular Actions in Cancer Gene Therapy
Mini-Reviews in Medicinal Chemistry Sphingolipid Metabolism Enzymes as Targets for Anti-Cancer Therapy
Current Drug Targets Tumour Reactions to Hypoxia
Current Molecular Medicine Aspirin: from a Historical Perspective
Recent Patents on Cardiovascular Drug Discovery Crosstalk of Long Non-coding RNAs and EMT: Searching the Missing Pieces of an Incomplete Puzzle for Lung Cancer Therapy
Current Cancer Drug Targets Editorial {Hot topic: QSPR Models for Computer-Aided Drug Design in Microbiology, Parasitology, and Pharmacology (Guest Editor: Humberto Gonzalez-Diaz)]
Current Computer-Aided Drug Design Doxycycline as Potential Anti-cancer Agent
Anti-Cancer Agents in Medicinal Chemistry