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海洋来源的博斯他汀衍生物的合成及其对肿瘤细胞的构效关系研究。

Studies on the synthesis of derivatives of marine-derived bostrycin and their structure-activity relationship against tumor cells.

机构信息

School of Chemistry and Chemical Engineering, Sun Yat-sen University, 135 Xingang West Road, Guangzhou 510275, China.

Guangdong Province Key Laboratory of Functional Molecules in Oceanic Microorganism, Bureau of Education, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou 510080, China.

出版信息

Mar Drugs. 2012 Apr;10(4):932-952. doi: 10.3390/md10040932. Epub 2012 Apr 24.

DOI:10.3390/md10040932
PMID:22690152
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3366684/
Abstract

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.

摘要

合成了一系列新型海洋来源的博斯他汀(1)衍生物(5-29)。采用 MTT 法测定了所有化合物对 MCF-7、MDA-MB-435、A549、HepG2、HCT-116 和 MCF-10A 细胞的体外细胞毒性。总共有 7、8、22、23、25、28 和 29 个化合物对所选癌细胞系的活性与阳性对照表阿霉素相当。然而,这些化合物对 MCF-10A 细胞也表现出细胞毒性。还根据获得的实验数据讨论了博斯他汀衍生物的构效关系(SAR)。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/3366684/60389830eb0f/marinedrugs-10-00932-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/3366684/a66ded491857/marinedrugs-10-00932-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/3366684/ad54ad893265/marinedrugs-10-00932-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/3366684/2a308a8defaa/marinedrugs-10-00932-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/3366684/3d9a3eeffc59/marinedrugs-10-00932-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/3366684/33e938395e99/marinedrugs-10-00932-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/3366684/60389830eb0f/marinedrugs-10-00932-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/3366684/a66ded491857/marinedrugs-10-00932-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/3366684/ad54ad893265/marinedrugs-10-00932-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/3366684/2a308a8defaa/marinedrugs-10-00932-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/3366684/3d9a3eeffc59/marinedrugs-10-00932-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/3366684/33e938395e99/marinedrugs-10-00932-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0a8/3366684/60389830eb0f/marinedrugs-10-00932-g006.jpg

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