Synthesis,biological evaluation and molecular docking studies of bis-chalcone derivatives as xanthine oxidase inhibitors and anticancer agents |
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| Institution: | 1. Tercan Vocational High School, Erzincan Binali Yildirim University, Erzincan 24800, Turkey;2. Deparment of Chemistry, Faculty of Science, Ataturk University, Erzurum 25240, Turkey;3. Department of Chemistry, Faculty of Science and Arts, ?nönü University, Malatya 44280, Turkey;4. Bioinformatics and Genetics Department, Faculty of Engineering and Natural Sciences, Kadir Has University, Istanbul 34083, Turkey;5. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mersin University, Mersin 33169, Turkey;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. Biotechnology Institute, Ankara University, Ankara 06110 Turkey;2. Department of Chemistry, Faculty of Science, Atatürk University, Erzurum 25240 Turkey;3. Tercan Vocational High School, Erzincan University, Erzincan 24800 Turkey;4. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Ankara 06110 Turkey;5. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mersin University, Mersin 33169 Turkey;1. Tercan Vocational High School, Erzincan Binali Yildirim University, Erzincan 24800, Turkey;2. Department of Chemistry, Faculty of Science, Atatürk University, Erzurum 25240, Turkey;3. Department of Pharmaceutical Basic Sciences, Faculty of Pharmacy, Erzincan Binali Yildirim University, Erzincan 24100, Turkey;4. Central Research and Application Laboratory, Agri Ibrahim Cecen University, Agri 04100, Turkey;5. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mersin University, Mersin 33169, Turkey;1. Department of Chemistry, Purdue University, 560 Oval Drive, West Lafayette, IN 47907-2084, USA;2. Department of Chemistry and Biochemistry, Northern Kentucky University, Nunn Drive, Highland Heights, KY 41099-1905, USA;3. Department of Biochemistry, Purdue University, 175 South University Street, West Lafayette, IN 47907-2063, USA;1. Department of Pharmacognosy and Pharmaceutical Chemistry, Faculty of Medicine and Biomedical Sciences, University of Yaoundé I, P.O. Box. 1364, Yaoundé, Cameroon;2. Department of Chemistry, Faculty of Science, University of Yaounde I, Yaounde, Cameroon;3. Department of Biochemistry, Faculty of Science, University of Dschang, Dschang, Cameroon;4. Department of Food Engineering, Faculty of Engineering and Architecture, Kafkas University, Kars 36100, Turkey;5. Department of Chemistry, Faculty of Science, University of Dschang, Dschang, Cameroon;6. Department of Chemistry, Faculty of Sciences, Atatürk University, Erzurum 25240, Turkey |
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| Abstract: | In this study, a series of B-ring fluoro substituted bis-chalcone derivatives were synthesized by Claisen-Schmidt condensation reactions and evaluated for their ability to inhibit xanthine oxidase (XO) and growth inhibitory activity against MCF-7 and Caco-2 human cancer cell lines, in vitro. According to the results obtained, the bis-chalcone with fluoro group at the 2 (4b) or 2,5-position (4g) of B-ring were found to be potent inhibitors of the enzyme with IC50 values in the low micromolar range. The effects of these compounds were about 7 fold higher than allopurinol. The binding modes of the bis-chalcone derivatives in the active site of xanthine oxidase were explained using molecular docking calculations. Also, compound 4g and 4h showed in vitro growth inhibitory activity against a panel of two human cancer cell lines 1.9 and 6.8 μM of IC50 values, respectively. |
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| Keywords: | Bis-chalcone Synthesis Claisen-Schmidt condensation Inhibition Cytotoxicity |
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