Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs |
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| Affiliation: | 1. Institute of Drug Discovery and Development, Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, PR China;2. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, Shanghai 201203, PR China;1. Division of Research and Review 3, Office of Biotechnology Products, Center for Drug Evaluation and Research, U.S. Food and Drug Administration, 10903 New Hampshire Ave., Silver Spring, MD 20993, USA;2. Cancer Genetics and Comparative Genomics Branch, National Human Genome Research Institute, National Institutes of Health, 50 South Dr., Bethesda, MD 20892, USA;3. George Washington School of Medicine and Health Sciences, Ross Hall, 2300 Eye St. NW, Washington, DC 20037, USA;4. Intramural Administrative Branch, National Institute of Allergy and Infectious Diseases, National Institutes of Health, 5640 Fishers Ln., Rockville, MD 20892, USA;1. Key Laboratory of Marine Drugs, Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, Qingdao, 266003, China;2. Laboratory for Marine Drugs and Bioproducts, Qingdao National Laboratory for Marine Science and Technology, Qingdao, 266237, China;3. Center for High Performance Computing & System Simulation, Qingdao National Laboratory for Marine Science and Technology, Qingdao, 266100, China;4. Department of Pharmacy, Qingdao Hiserve Medical Center, Qingdao, 266003, China |
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| Abstract: | In an effort to discover potent antitumor agents, a series of novel C-7-heteroaryl-substituted camptothecin derivatives were designed and synthesized via microwave-promoted Suzuki coupling reaction. These analogs were then assessed for cytotoxicity against three human tumor cell lines, A549, HCT116, HT-29, and inhibitory effects on topoisomerase I. All of the new compounds showed potent inhibition of human tumor cell growth, among which compound 10a showed higher cytotoxic activity than that of SN-38. Furthermore, this series of compounds retained or enhanced Topo I inhibition. |
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| Keywords: | Camptothecin C-7-heteroaryl-substituted camptothecin Suzuki coupling Antitumor |
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