Synthesis,biological evaluation and molecular docking studies of a new series of chalcones containing naphthalene moiety as anticancer agents |
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| Institution: | 1. Provincial Key Laboratory of Pharmaceutics in Guizhou Province, Guizhou Medical University, Beijing Road, Guiyang 550004, China;2. School of Pharmacy, Guizhou Medical University, 4 Beijing Road, Guiyang 550004, China;3. National Engineering Research Center of Miao’s Medicines, 4 Beijing Road, Guiyang 550004, China;4. College of Chemistry and Chemical Engineering, Hunan Engineering Laboratory for Analyse and Drugs Development of Ethnomedicine in Wuling Mountains, Jishou University, Jishou 416000, China;1. School of Chemical Engineering and Materials Science, Chung-Ang University, Seoul, Republic of Korea;2. Department of Internal Medicine, Seoul National University, College of Medicine, Seoul, Republic of Korea;1. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Deraya University, Minia, Egypt;2. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt;3. Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Aljouf, Sakaka 2014, Saudi Arabia;4. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sohag University, 82524 Sohag, Egypt;5. Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, 61519 Minia, Egypt;1. Department of Chemistry, Faculty of Science, Srinakharinwirot University, Bangkok 10110, Thailand;2. Center of Data Mining and Biomedical Informatics, 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. Chulabhorn Research Institute, Bangkok 10210, Thailand;5. Program in Chemical Biology, Chulabhorn Graduate Institute, Bangkok 10210, Thailand;6. Center of Excellence on Environmental Health and Toxicology (EHT), CHE, Ministry of Education, Thailand;1. State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, China;2. College of Chemistry and Chemical Engineering, Jishou University, Jishou, China;3. College of Food Science and Technology, Shanghai Ocean University, Shanghai, China;4. Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang, China;5. School of Pharmacy, Guizhou Medical University, Guiyang, China;1. Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Horus University, New Dammeitta, Egypt;3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Delta University, Gamsaa, Egypt |
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| Abstract: | A series of chalcones containing naphthalene moiety 4a–4p have been synthesized, characterized by 1H NMR and 13C NMR and evaluated for their in vitro anticancer activity. The majority of the screened compounds displayed potent anticancer activity against both HCT116 and HepG2 human cancer cell lines. Among the series, compound 4h with a diethylamino group at the para position of the phenyl ring exhibited the most potent anticancer activity against HCT116 and HepG2 cell lines with IC50 values of 1.20 ± 0.07 and 1.02 ± 0.04 μM, respectively. The preliminary structure–activity relationship has been summarized. Tubulin polymerization experiments indicated that 4h effectively inhibited tubulin polymerization and flow cytometric assay revealed that 4h arrests HepG2 cells at the G2/M phase in a dose-dependent manner. Furthermore, molecular docking studies suggested that 4h binds to the colchicine binding site of tubulin. |
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| Keywords: | Anticancer activity Tubulin inhibitor Chalcone Naphthalene |
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