Journal
MARINE DRUGS
Volume 10, Issue 4, Pages 932-952Publisher
MDPI
DOI: 10.3390/md10040932
Keywords
bostrycin; synthesis; antitumor; derivatives; structure-activity relationship
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Funding
- National Natural Science Foundation of China [20972197, 41176128]
- 863 Foundation of China [2011AA09070201]
- Key Science and Technique Research Project of Guangdong Province of China [2010B030600003, 2010B030600004, 2011A080403006]
- National Science and Technique Major Project [2012ZX09102-101-017]
- University-industry Cooperation Projects of Guangdong Province
- Ministry of Education [2008B090500171]
- Guangzhou Project of Science & Technology Planning [2010J1-E331]
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A series of new derivatives (5-29) of marine-derived bostrycin (1) were synthesized. The in vitro cytotoxic activities of all compounds were evaluated against MCF-7, MDA-MB-435, A549, HepG2, HCT-116 and MCF-10A cells using the MTT method. The compounds 7, 8, 22, 23, 25, 28 and 29 of the total showed comparable activity to epirubicin, the positive control, against the tested cancer cell lines. However, these compounds also exhibited cytotoxicity towards MCF-10A cells. The structure-activity relationship (SAR) of bostrycin derivatives was also discussed based on the obtained experimental data.
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