Synthesis,cytotoxicity, and in vivo antitumor activity study of parthenolide semicarbazones and thiosemicarbazones |
| |
| Affiliation: | 1. School of Chemical Engineering, Beijing Institute of Petrochemical Technology, Beijing 102617, PR China;2. State Key Laboratory of Bioactive Substance and Function of Natural Medicines and Beijing Key Laboratory of Active Substances Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China;3. Beijing Key Laboratory of Enze Biomass Fine Chemicals, Beijing Institute of Petrochemical Technology, Beijing 102617, PR China;1. Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China;2. Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China;1. Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University, Seoul 02447, Republic of Korea;2. Department of Life and Nanopharmaceutical Science, College of Pharmacy, Kyung Hee University, Seoul 02447, Republic of Korea;3. Department of Physiology and Pharmacology, Hotchkiss Brain Institute and Alberta Children’s Hospital Research Institute, Cumming School of Medicine, University of Calgary, Calgary T2N 4N1, Canada;4. KHU-KIST Department of Converging Science and Technology, Kyung Hee University, Seoul 02447, Republic of Korea;1. Department of Basic Medicinal Sciences, Graduate School of Pharmaceutical Sciences, Nagoya University, Furo-cho, Chikusa-ku, Nagoya 464-8601, Japan;2. Laboratory for Chemistry and Life Science, Institute of Innovative Research, Tokyo Institute of Technology, 4259 Nagatsuta-cho, Midori-ku, Yokohama 226-8503, Japan;3. School of Life Science and Technology, Tokyo Institute of Technology, 4259 Nagatsuta-cho, Midori-ku, Yokohama 226-8503, Japan;1. Department of Chemistry, Mahatma Gandhi College, University of Kerala, Thiruvananthapuram, 695 004, Kerala, India;2. Department of Chemistry, Faculty of Science, Eastern University, Chenkalady, Sri Lanka;3. Department of Chemistry, Sree Narayana College, Chempazhanthy, Thiruvananthapuram, 695 587, Kerala, India;1. Department of Pharmaceutics, State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 211198, China;2. Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing 210023, China;3. Clinical Medical Laboratory Center, Jining No. 1 People''s Hospital, Jining, Shandong 272000, China |
| |
| Abstract: | Parthenolide is an important sesquiterpene lactone with potent anticancer activities. In order to further improve its biological activity, a series of parthenolide semicarbazone or thiosemicarbazone derivatives was synthesized and evaluated for their anticancer activity. Derivatives were tested in vitro against 5 human tumor cell lines, and many of these showed higher cytotoxicity than parthenolide. Five compounds were further studied for their antitumor activity in mice. The in vivo result indicated that compound 4d showed both promising antitumor activity against mice colon tumor and small side effects on immune systems. The cell apoptosis and cell cycle distribution of compound 4d were also studied. Molecular docking studies revealed multiple interactions between 4d and NF-κB. Our findings demonstrate the potential of semicarbazones as a promising type of compounds with anticancer activity. |
| |
| Keywords: | Anticancer Parthenolide Semicarbazone |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
