Synthesis and anticancer activity of open-resorcinarene conjugates |
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| Affiliation: | 1. Instituto de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, Circuito Exterior, Coyoacán, C.P 04510 México, D.F., Mexico;2. Facultad de Química, Universidad Nacional Autónoma de México, Ciudad Universitaria, Circuito Interior, Coyoacán, C.P 04510 México, D.F., Mexico;1. China International Science and Technology Cooperation Base of Food Nutrition/Safety and Medicinal Chemistry, College of Biotechnology, Tianjin University of Science & Technology, Tianjin 300457, China;2. School of Pharmacy, Tianjin Medical University, Tianjin 300070, China;3. Centre de recherche de Gif-sur-Yvette, Institut de Chimie des Substances Naturelles, UPR 2301, CNRS, Avenue de la Terrasse, 91198 Gif-sur-Yvette, France;1. Division of Crop Foundation, National Institute of Crop Science (NICS), Rural Development Administration (RDA), Wanju 55365, Republic of Korea;2. Department of Crop Science and Biotechnology, Dankook University, Cheonan 31116, Republic of Korea;3. Department of Biological Sciences, Chonbuk National University, Jeonju 54896, Republic of Korea;4. Forest Biomaterials Research Center, National Institute of Forest Science (NIFS), Jinju 52817, Republic of Korea;1. Centre of Excellence for Pharmaceutical Sciences, School of Pharmacy, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa;2. Human Metabolomics, Faculty of Natural and Agricultural Science, North-West University, Private Bag X6001, Box 269, Potchefstroom 2531, South Africa;3. Pharmaceutical Chemistry, School of Pharmacy, North-West University, Private Bag X6001, Potchefstroom 2520, South Africa;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 |
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| Abstract: | The first example of conjugation of open-resorcinarenes with chlorambucil, ibuprofen, naproxen and indomethacin are presented. The cytotoxic properties of the obtained conjugates were tested against the cancer cell lines U-251, PC-3, K-562, HCT-15, MCF-7 and SKLU-1. It was found that the conjugate with chlorambucil, naproxen or indomethacin (having 8 moieties) was toxic towards cancer cell lines U-251 and K-562, with no activity against non-cancerous COS-7 cells. The conjugates with naproxen and indomethacin showed high selectivity towards U-251 tumor cells. |
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| Keywords: | Open-resorcinarene Dendrimers Anticancer activity Nonsteroidal anti-inflammatory drugs Chlorambucil |
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