Facile synthesis of novel substituted aryl-thiazole (SAT) analogs via one-pot multi-component reaction as potent cytotoxic agents against cancer cell lines |
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| Institution: | 1. H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan;2. Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan;3. Department of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah 21412, Saudi Arabia;1. Department of Organic Chemistry, University of Madras, Guindy Campus, Chennai, India;2. Institute of Molecular and Cell Biology (IBMC), University of Strasbourg, Strasbourg, France;3. Department of Inorganic Chemistry, University of Madras, Guindy Campus, Chennai, India;1. School of Chemical Sciences, Swami Ramanand Teerth Marathwada University, Nanded, MH 431606, India;2. School of Life Sciences, Swami Ramanand Teerth Marathwada University, Nanded, MH 431606, India;1. Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmacy, Shanghai Jiao Tong University, No. 800 Dongchuan Rd., Minhang District, Shanghai 200240, PR China;2. SJTU-Agilent Technologies Joint Laboratory for Pharmaceutical Analysis, School of Pharmacy, Shanghai Jiao Tong University (SJTU), No. 800 Dongchuan Rd., Minhang District, Shanghai 200240, PR China;1. Department of Chemical Technology and Pharmaceuticals, Faculty of Pharmacy, Collegium Medicum, Nicolaus Copernicus University, Jurasza 2, 85-089, Bydgoszcz, Poland;2. Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Rudolfa Weigla 12, 53-114, Wrocław, Poland;3. Institute of Physics, Kazimierz Wielki University, Plac Weyssenhoffa 11, 85-072, Bydgoszcz, Poland;4. Department of Organic Chemistry, Faculty of Pharmacy, Medical University, Chodźki 4a, 20-093, Lublin, Poland;5. Institute of Chemistry, University of Silesia, Szkolna 9, 40-006, Katowice, Poland;6. A. Chełkowski Institute of Physics, University of Silesia, Uniwersytecka 4, Katowice, 40-007, Poland;7. Silesian Center for Education and Interdisciplinary Research, 75 Pulku Piechoty 1A, Chorzów, 41-500, Poland;8. Faculty of Chemical Technology and Engineering, University of Technology and Life Sciences, Seminaryjna 3, 85-326, Bydgoszcz, Poland;1. Sigma-Aldrich Chemical Pvt. Ltd., Bommasandra-Jigani Link Road, Bengaluru, 560100, India;2. Department of Chemistry, Canara Engineering College, Benjanapadavu, Mangaluru, 574219, India;3. Department of Chemistry, St Joseph Engineering College, Vamanjoor, Mangaluru, 575005, India;4. DST-PURSE Lab., Mangalagangotri, Mangalore University, Mangaluru, 574199, India;5. Department of Materials Science, Mangalagangotri, Mangalore University, Mangaluru, 574199, India;6. Department of Chemistry, Sahyadri Science College, Shimoga, 577 201, India;7. Department of Chemistry, Nagarjuna College of Engineering and Technology, Bengaluru, 562164, India |
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| Abstract: | In this study, twenty-five (25) substituted aryl thiazoles (SAT) 1–25 were synthesized, and their in vitro cytotoxicity was evaluated against four cancer cell lines, MCF-7 (ER+ve breast), MDA-MB-231 (ER−ve breast), HCT116 (colorectal) and HeLa (cervical). The activity was compared with the standard anticancer drug doxorubicin (IC50 = 1.56 ± 0.05 μM). Among them, compounds 1, 4–8, and 19 were found to be toxic to all four cancer cell lines (IC50 values 5.37 ± 0.56–46.72 ± 1.80 μM). Compound 20 was selectively active against MCF7 breast cancer cells with IC50 of 40.21 ± 4.15 μM, whereas compound 19 was active against MCF7 and HeLa cells with IC50 of 46.72 ± 1.8, and 19.86 ± 0.11 μM, respectively. These results suggest that substituted aryl thiazoles 1 and 4 deserve to be further investigated in vivo as anticancer leads. |
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| Keywords: | Thiazole Characterization Anticancer agents (MCF7 MDA-MB-231) (HCT-116) (HeLa) Cytotoxicity |
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