Synthesis of diethylamino-curcumin mimics with substituted triazolyl groups and their sensitization effect of TRAIL against brain cancer cells |
| |
| Institution: | 1. Department of Hematology and oncology, Gangneung Asan Hospital, University of Ulsan College of Medicine, Gangneung 210-711, Republic of Korea;2. Department of Basic Science, Kwandong University College of Medicine, Gangneung 210-701, Republic of Korea;3. Department of physiology, Kwandong University College of Medicine, Gangneung 210-701, Republic of Korea;4. Department of Microbiology, Kwandong University College of Medicine, Gangneung 210-701, Republic of Korea;5. Department of Surgery, Gangneung Asan Hospital, University of Ulsan College of Medicine, Gangneung 210-711, Republic of Korea;6. Department of Neurosurgery, Gangneung Asan Hospital, University of Ulsan College of Medicine, Gangneung 210-711, Republic of Korea;7. Department of Pharmacology, Kwandong University College of Medicine, Gangneung 210-701, Republic of Korea;1. Institute of Chinese Medical Sciences, State Key Laboratory of Quality Research in Chinese Medicine, University of Macau, Av. Padre Tomás Pereira S.J., Taipa, Macao 999078, China;2. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Xueyuan Rd., Haidian District, 100191, Beijing, China;3. Molecular Oncology Laboratory, University of Chicago Medical Center, 5841 South Maryland Av., MC 3079, Chicago, IL 60637, USA;4. Institute of Materia Medica, Zhejiang Chinese Medical University, 548 Binwen Rd., Binjiang District, 310053, Zhejiang, China;1. Department of Chemistry, Faculty of Science, Srinakharinwirot University, Bangkok 10110, Thailand;2. Center for Research and Innovation, Faculty of Medical Technology, Mahidol University, Bangkok 10700, Thailand;3. Department of Clinical Microbiology and Applied Technology, Faculty of Medical Technology, Mahidol University, Bangkok 10700, Thailand;4. Center of Data Mining and Biomedical Informatics, Faculty of Medical Technology, Mahidol University, Bangkok 10700, Thailand;5. Chulabhorn Research Institute, Bangkok 10210, Thailand;6. Program in Chemical Biology, Chulabhorn Graduate Institute, Bangkok 10210, Thailand;7. Center of Excellence on Environmental Health and Toxicology (EHT), CHE, Ministry of Education, Thailand;1. Medicinal Chemistry and Pharmacology, CSIR - Indian Institute of Chemical Technology, Hyderabad 500007, India;2. Centre for Chemical Biology, CSIR - Indian Institute of Chemical Technology, Hyderabad 500007, India;3. Anti-Cancer Drug Screening Facility (ACDSF), Advanced Centre for Treatment, Research & Education in Cancer (ACTREC), Tata Memorial Centre, Kharghar, Navi Mumbai 410210, India;1. Department of Chemistry and Biochemistry, University of Minnesota Duluth, Duluth, MN 55812, United States;2. Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN 55812, United States;3. Department of Pharmacy Practice & Pharmaceutical Sciences, University of Minnesota, Duluth, MN 55812, United States |
| |
| Abstract: | A newly designed curcumin mimic library (11a–11k) with 2-ethylamino groups in a chalcone structure and variously substituted triazole groups as side chains was synthesized using the Huisgen 1,3-cycloaddition reaction between various alkynes (a–k) and an intermediate (10), with CuSO4 and sodium ascorbate in a solution mixture of chloroform, ethanol, and water (5:3:1) at room temperature for 5 h. In the lactate dehydrogenase (LDH) release assay involving co-treatment with tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) and/or synthetic curcumin derivatives using TRAIL-resistant human CRT-MG astroglioma cells, the novel curcumin mimic library was found to effectively stimulate the cytotoxicity of TRAIL, causing mild cytotoxicity when administered alone. In particular, 11a and 11j are promising candidates for TRAIL-sensitizers with potential use in combination chemotherapy for brain tumors. |
| |
| Keywords: | Curcumin TRAIL Anticancer Curcumin mimics Brain tumor |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
