Synthesis and evaluation of novel sulfonamide analogues of 6/7-aminoflavones as anticancer agents via topoisomerase II inhibition |
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| Institution: | 1. Department of Chemistry, Prof John Barnabas Post Graduate School of Biological Studies, Ahmednagar College, Ahmednagar, Ahmednagar 414001, India;2. Department of Chemistry, Deogiri College, Station Road, Aurangabad 431 005, MS, India;3. Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431 004, MS, India;4. Department of Pharmaceutical Chemistry, R C Patel Institute of Pharmaceutical Education & Research, Shirpur 425405, MS, India;5. Department of Pharmaceutical Chemistry, Durgamata Institute of Pharmacy, Dharmapuri, Parbhani 431401, MS, India;6. Department of Animal Biology, University of Hyderabad, Hyderabad, 500046, India;1. Department of Chemistry, Physics, and Atmospheric Sciences, Jackson State University, Jackson, MS 39217, USA;2. Department of Biochemistry, Federal University of Technology, Akure, Nigeria;1. Department of Nuclear Medicine, The Affiliated Hospital of Qingdao University, Qingdao 266000, PR China;2. Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing 100142, PR China;3. Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Biochemistry and Molecular Biology, Peking University Cancer Hospital & Institute, Beijing 100142, PR China;1. Department of Chemistry, Deogiri College, Aurangabad 431 005, Maharashtra, India;2. Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad 431 004, Maharashtra, India;3. Department of Pharmaceutical Chemistry, Durgamata Institute of Pharmacy, Dharmapuri, Parbhani 431401, MS, India;4. Department of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education & Research, Shirpur 425405, MS, India;5. Dr. Prabhakar Kore Basic Science Research Center, KLE Academy of Higher Education and Research, Nehru Nagar, Belagavi 590010, Karnataka, India;6. KLE College of Pharmacy, KLE Academy of Higher Education and Research, Nehru Nagar, Belagavi 590010, Karnataka, India;7. Department of Biotechnology, KLEF University, Vaddeswaram, AP 522502, India;1. Department for Life Quality Studies, Alma Mater Studiorum-Università di Bologna, Corso D’Augusto 237, 47921, Rimini, Italy;2. Molecular Modeling and Drug Discovery Lab, Istituto Italiano di Tecnologia, Via Morego 30, 16163, Genova, Italy;3. Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Via Marzolo, 5, 35131, Padova, Italy;4. Department of Drug Science and Technology, University of Turin, Via Giuria 9, 10125, Torino, Italy;5. Department of Industrial Chemistry “Toso Montanari”, Alma Mater Studiorum-Università di Bologna, Viale Del Risorgimento, 4, 40136, Bologna, Italy;6. Cell Death Investigation and Therapy Laboratory, Department of Human Structure and Repair, Ghent University, 9000, Ghent, Belgium;7. Cancer Research Institute Ghent, 9000, Ghent, Belgium;8. Department of Pathophysiology, Sechenov First Moscow State Medical University (Sechenov University), 119146 Moscow, Russia;9. Department of Biomolecular Sciences, Campus Scientifico “E. Mattei”, University of Urbino Carlo Bo, Via Ca’ Le Suore 2, Urbino, Italy |
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| Abstract: | A series of new sulfonamide analogues of 6/7-aminoflavones were synthesized by using molecular hybridization approach. These new sulfonamide analogues were screened for antiproliferative activity against human hepatocellular carcinoma (HepG-2), human lung cancer cell line (A-549), human colorectal adenocarcinoma (Caco-2) cancer cell lines. Compounds 5p, 5q, 5t, 5v, 5w and 5x exhibited good anticancer activity against selected cancer cell lines. These compounds were further evaluated to predict their ability to inhibit topoisomerase-II enzyme. Compound 5x has shown potent antiproliferative activity (IC50 value 0.98 µM) as compared to standard drug Adriamycin (IC50 = 0.94 µM) indicating that these compounds exhibits anticancer activity via inhibition of topoisomerase-II enzyme. Docking results also have supported above observations by indicating that compounds are held in the active pocket by combination of various hydrogen and hydrophobic interactions with Top II-DNA-etoposide enzyme. |
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| Keywords: | Aminoflavones Sulfonamide Docking Anticancer activity topoisomerase-II |
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