Synthesis and anti-proliferative activity of a novel 1,2,3-triazole tethered chalcone acetamide derivatives |
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| Institution: | 1. Fluoro-Agrochemicals Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India;2. Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India;3. Centre for Molecular Modeling, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India;1. Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, Punjab, India;2. Department of Medicine, University of California, San Francisco, CA, USA;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. Department of Chemistry, Guru Jambheshwar University of Science & Technology, Hisar, Haryana, 125001, India;2. Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science & Technology, Hisar, Haryana, 125001, India;3. Department of Chemistry, National Institute of Technology, Kurukshetra, Haryana, 136119, India;1. Department of Physics, DDU Gorakhpur University, Gorakhpur, 273009, India;2. Department of Physics, B.R.D. P.G. College, Deoria, 274001, India;1. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran;2. Department of Medicinal Chemistry, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Iran;3. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Research Institute, Tehran University of Medical Sciences, Tehran, Iran;4. Department of Medicinal Chemistry, School of Pharmacy-International Campus, Iran University of Medical Sciences, Tehran, Iran;5. Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran;6. Department of Cellular Biotechnology at Cell Science Research Center, Royan Institute for Biotechnology, ACECR, Isfahan, Iran;7. Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran;8. Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran |
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| Abstract: | A new series of 1,2,3-triazole tethered chalcone acetamide derivatives (7a-c & 8a-r) have been synthesized in excellent yields and their structures were determined by analytical and spectral (FT-IR, 1H NMR, 13C NMR & HRMS) studies. The newly synthesized derivatives were evaluated for their cytotoxic activity against four human cancer cell lines, such as HeLa (Human cervical cancer), A549 (Human alveolar adenocarcinoma), MCF-7 (Human breast adenocarcinoma) and SKNSH (Human brain cancer). Among them, compound 7c exhibited good anti-proliferation activity with HeLa (IC50 7.41 + 0.8 μM), SKNSH (IC50 8.68 + 1.1 μM), MCF-7 (IC50 9.76 + 1.3 μM) and MDA-MB-231, while compounds 7a and 7b showed promising anti-proliferation against above four human cancer cell lines with IC50 7.95–11.62 μM, respectively, compared with the standard drug Doxorubicin. We explored the probable key active site and binding mode interactions in HDAC8 (PDB ID:3SFH) and EHMT2 (PDB ID:3K5K) proteins. The docking results are complementary to the experimental observations. |
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| Keywords: | Chalcone Acetamides Cytotoxicity Jones reagent Growth inhibition Human cancer cell lines |
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