Abstract
The 2-amino-6-trifluoromethyl-3H-pyrimidin-4-one 1 was propargylated to give two regioisomers 2, 3 in definite proportions. Both regioisomers 2 and 3 were independently reacted with alkyl, aryl or cycloalkyl substituted azides under Sharpless conditions and were obtained exclusively 1,4–disubstituted triazole tagged trifluoromethyl substituted pyrimidine derivatives 4 and 5 respectively. All the final products were evaluated for cytotoxic activity against four cancer cell lines and promising compounds were identified.
Keywords: Alkylation, Propargyl bromide, 3H-pyrimidin-4-one, Regioisomers, Sharpless conditions, Triazoles.
Letters in Drug Design & Discovery
Title:Studies on Synthesis of Novel Triazolalkyl Tagged Trifluoromethyl Substituted Pyrimidine Derivatives and their Evaluation for Cytotoxic Activity
Volume: 10 Issue: 9
Author(s): Punna Nagender, Gannarapu Malla Reddy, Royya Naresh Kumar, Anugu Chandrashekar Reddy, Loka Reddy Velatooru, Rajesh Pamanji, Janapala Venkateswara Rao and Banda Narsaiah
Affiliation:
Keywords: Alkylation, Propargyl bromide, 3H-pyrimidin-4-one, Regioisomers, Sharpless conditions, Triazoles.
Abstract: The 2-amino-6-trifluoromethyl-3H-pyrimidin-4-one 1 was propargylated to give two regioisomers 2, 3 in definite proportions. Both regioisomers 2 and 3 were independently reacted with alkyl, aryl or cycloalkyl substituted azides under Sharpless conditions and were obtained exclusively 1,4–disubstituted triazole tagged trifluoromethyl substituted pyrimidine derivatives 4 and 5 respectively. All the final products were evaluated for cytotoxic activity against four cancer cell lines and promising compounds were identified.
Export Options
About this article
Cite this article as:
Nagender Punna, Reddy Malla Gannarapu, Kumar Naresh Royya, Reddy Chandrashekar Anugu, Velatooru Reddy Loka, Pamanji Rajesh, Rao Venkateswara Janapala and Narsaiah Banda, Studies on Synthesis of Novel Triazolalkyl Tagged Trifluoromethyl Substituted Pyrimidine Derivatives and their Evaluation for Cytotoxic Activity, Letters in Drug Design & Discovery 2013; 10 (9) . https://dx.doi.org/10.2174/1570180811310090010
DOI https://dx.doi.org/10.2174/1570180811310090010 |
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
-
Classifications and Clinical Assessment of Haemorrhoids: The Proctologist’s Corner
Reviews on Recent Clinical Trials Targeting the Epidermal Growth Factor Pathway as Therapy for Glioblastoma
Current Cancer Therapy Reviews (Section A: Molecular, Structural, and Cellular Biology of Drug Transporters) The Role of MDR1 Genetic Polymorphisms in Interindividual Variability in P-glycoprotein Expression and Function
Current Drug Metabolism Targeting Stem Cells-Clinical Implications for Cancer Therapy
Current Stem Cell Research & Therapy Artificial O2 Carriers: Status in 2005
Current Pharmaceutical Design An Overview of Bioactive Peptides for in vivo Imaging and Therapy in Human Diseases
Mini-Reviews in Medicinal Chemistry Platinum Formulations as Anticancer Drugs Clinical and Pre-Clinical Studies
Current Topics in Medicinal Chemistry Developing Histone Deacetylase Inhibitors as Anti-Cancer Therapeutics
Current Medicinal Chemistry Episensitization: Therapeutic Tumor Resensitization by Epigenetic Agents: A Review and Reassessment
Anti-Cancer Agents in Medicinal Chemistry QSAR Multi-Target in Drug Discovery: A Review
Current Computer-Aided Drug Design Short-Chain Fatty Acid Inhibitors of Histone Deacetylases: Promising Anticancer Therapeutics?
Current Cancer Drug Targets Anti-Angiogenic Therapy: Strategies to Develop Potent VEGFR-2 Tyrosine Kinase Inhibitors and Future Prospect
Current Medicinal Chemistry Prevention and Treatment for Chemotherapy-Induced Peripheral Neuropathy: Therapies Based on CIPN Mechanisms
Current Neuropharmacology Recent Advances in Colon Drug Delivery Technology
Drug Delivery Letters Natural Compounds with Proteasome Inhibitory Activity for Cancer Prevention and Treatment
Current Protein & Peptide Science Mitophagy in Carcinogenesis and Tumour Progression- A New Paradigm with Emerging Importance
Anti-Cancer Agents in Medicinal Chemistry Molecular Processes in Cancers and Cancer Chemotherapy
Current Chemical Biology Direct Selection of cDNAs from Filamentous Phage Surface Display Libraries: An Update
Medicinal Chemistry Reviews - Online (Discontinued) S-equol, a Secondary Metabolite of Natural Anticancer Isoflavone Daidzein, Inhibits Prostate Cancer Growth In Vitro and In Vivo, Though Activating the Akt/FOXO3a Pathway
Current Cancer Drug Targets Histone Deacetylase Inhibitors: New Promise in the Treatment of Immune and Inflammatory Diseases
Current Drug Targets