Abstract
21 new structures of isoxazole-moiety-containing thieno[2,3-d]pyrimidine derivatives(3a~3u) were synthesized for the first time and characterized using IR, 1H NMR, 13C NMR, ESI-MS and elemental analysis techniques. And then their in vitro anticancer activity against lung cancer A549, colorectal HCT116 and breast cancer MCF-7 cell lines was preliminarily evaluated using the MTT method. Among them, most compounds exhibited good to excellent anticancer activity. In particular, 3g, 3j and 3n exhibited a broad spectrum and more potent anticancer activity against A549, HCT116 and MCF-7 cell lines, which can be regarded as the promising anticancer drug-candidates.
Keywords: Anticancer activity, isoxazole moiety, synthesis, thieno[2, 3-d]pyrimidine derivatives.
Anti-Cancer Agents in Medicinal Chemistry
Title:Synthesis of Isoxazole Moiety Containing Thieno[2,3-d]pyrimidine Derivatives and Preliminarily in vitro Anticancer Activity (Part II)
Volume: 15 Issue: 9
Author(s): Jianping Yong, Canzhong Lu and Xiaoyuan Wu
Affiliation:
Keywords: Anticancer activity, isoxazole moiety, synthesis, thieno[2, 3-d]pyrimidine derivatives.
Abstract: 21 new structures of isoxazole-moiety-containing thieno[2,3-d]pyrimidine derivatives(3a~3u) were synthesized for the first time and characterized using IR, 1H NMR, 13C NMR, ESI-MS and elemental analysis techniques. And then their in vitro anticancer activity against lung cancer A549, colorectal HCT116 and breast cancer MCF-7 cell lines was preliminarily evaluated using the MTT method. Among them, most compounds exhibited good to excellent anticancer activity. In particular, 3g, 3j and 3n exhibited a broad spectrum and more potent anticancer activity against A549, HCT116 and MCF-7 cell lines, which can be regarded as the promising anticancer drug-candidates.
Export Options
About this article
Cite this article as:
Yong Jianping, Lu Canzhong and Wu Xiaoyuan, Synthesis of Isoxazole Moiety Containing Thieno[2,3-d]pyrimidine Derivatives and Preliminarily in vitro Anticancer Activity (Part II), Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (9) . https://dx.doi.org/10.2174/1871520615666150305103122
DOI https://dx.doi.org/10.2174/1871520615666150305103122 |
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
-
Aminophosphonate Metal Complexes of Biomedical Potential
Current Medicinal Chemistry Intersection of MicroRNA and Gene Regulatory Networks and their Implication in Cancer
Current Pharmaceutical Biotechnology Restoration of Antitumor Immunity Through Selective Inhibition of Myeloid Derived Suppressor Cells by Anticancer Therapies
Current Molecular Medicine Protein Tyrosine Signaling and its Potential Therapeutic Implications in Carcinogenesis
Current Pharmaceutical Design Cholecystokinin-2 Receptor Targeting with Radiolabeled Peptides: Current Status and Future Directions
Current Medicinal Chemistry Mesenchymal Stem Cell Therapy in Intracerebral Haemorrhagic Stroke
Current Medicinal Chemistry Design, Synthesis and Pharmacological Evalution of 1,3,4-Oxadiazole Derivatives as Collapsin Response Mediator Protein 1 (CRMP 1) Inhibitors
Current Drug Discovery Technologies Are KRAS/BRAF Mutations Potent Prognostic and/or Predictive Biomarkers in Colorectal Cancers?
Anti-Cancer Agents in Medicinal Chemistry Pluripotent Stem Cells for Livestock Health and Production
Current Stem Cell Research & Therapy Changes in Glutathione, Oxidative Stress and Mitochondrial Membrane Potential in Apoptosis Involving the Anticancer Activity of Cantharidin Isolated from Redheaded Blister Beetles, Epicauta hirticornis
Anti-Cancer Agents in Medicinal Chemistry The Role of CXC-Chemokine IL-8, IL-6 and CXCR2 Receptor in Lymphoplasmacytic Lymphoma: Correlations with Microvascular Characteristics and Clinical Features
Current Angiogenesis (Discontinued) Can Targeted Therapy be Successful without Metronomic Scheduling ?
Current Topics in Medicinal Chemistry Hemopoiesis in Ph-Negative Chronic Myeloproliferative Disorders
Current Stem Cell Research & Therapy Therapeutic Challenges in Neuroendocrine Tumors
Anti-Cancer Agents in Medicinal Chemistry Peptide-Based Anticancer Vaccines: Recent Advances and Future Perspectives
Current Medicinal Chemistry The Typical Metabolic Modifiers Conferring Improvement in Cancer Resistance
Current Medicinal Chemistry Apoptosis and Autophagy Induction As Mechanism of Cancer Prevention by Naturally Occurring Dietary Agents
Current Drug Targets Single-Cell Sequencing for Drug Discovery and Drug Development
Current Topics in Medicinal Chemistry How Cancer Cells Resist Chemotherapy: Design and Development of Drugs Targeting Protein-Protein Interactions
Current Topics in Medicinal Chemistry Tumor Dormancy and the Angiogenic Switch: Possible Implications of Bone Marrow- Derived Cells
Current Pharmaceutical Design