Synthesis and antitumor evaluation of methyl spongoate analogs |
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| Authors: | Cheng-Shi Jiang Cai-Guo Huang Bo Feng Jia Li Jing-Xu Gong Tibor Kurtán Yue-Wei Guo |
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| Institution: | 1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhang Jiang High-Tech Park, Shanghai 201203, PR China;2. Second Military Medical University, 800 Xiang Yin Road, Shanghai 200433, PR China;3. Department of Organic Chemistry, University of Debrecen, PO Box 20, 4010 Debrecen, Hungary;1. JADO Technologies, Tatzberg 47-51, 01307 Dresden, Germany;2. Department of Chemistry, Technische Universität Dresden, Bergstr. 66, 01069 Dresden, Germany;3. Max Planck Institute for Molecular Cell Biology and Genetics, 01307 Dresden, Germany;4. Institute of Anatomy, Technische Universität Dresden, Fiedlerstr. 42, 01307 Dresden, Germany;1. Department of Chemistry, Islamia College of Science and Commerce, Srinagar 190009, India;2. Department of Chemistry and Biochemistry, University of Arizona, Tucson 85721, USA;1. Institute of Chemistry, Academia Sinica, Taipei 115, Taiwan;2. Doctoral Degree Program in Marine Biotechnology, National Sun Yat-Sen University, Kaohsiung 804, Taiwan;1. Department of Chemistry, Islamia College of Science and Commerce, Srinagar 190009, India;2. Department of Chemistry and Biochemistry, University of Arizona, Tucson 85721, USA;3. Department of Chemistry, University of Kashmir, Hazratbal, Srinagar 190002, India;1. Department of Organic Chemistry, University of Szeged, Dóm tér 8, H-6720 Szeged, Hungary;2. Department of Pharmacodynamics and Biopharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary;3. Cereal Research Non-Profit LTD, P.O. Box 391, H-6701 Szeged, Hungary;4. Virtua Drug Ltd, Csalogány u. 4C, H-1015 Budapest, Hungary |
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| Abstract: | A series of novel methyl spongoate (1) analogs has been synthesized and evaluated for their in vitro cytotoxic properties. It was found that the nature of the C-20 side chain had significant effects on their bioactivities and some analogs showed higher cytotoxicity than 1 against A549, HCT-116, HepG2, SW-1990, MCF-7 and NCI-H460 tumor cell lines. The pharmacological results confirmed that the α,β-unsaturated carbonyl moiety, a Michael acceptor in ring A, plays a pivotal role in the cytotoxic effect of these derivatives. The compiled pharmacological data may be useful for the design of novel analogous anticancer drugs. |
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