Studies on the Synthesis of Derivatives of Marine-Derived Bostrycin and Their Structure-Activity Relationship against Tumor Cells

Author： Chen Hong   Zhong Lili   Long Yuhua   Li Jia   Wu Jueheng   Liu Lan   Chen Shengping   Lin Yongcheng   Li Mengfeng   Zhu Xun   She Zhigang  

Publisher： MDPI

E-ISSN： 1660-3397|10|4|932-952

ISSN： 1660-3397

Source： Marine Drugs, Vol.10, Iss.4, 2012-04, pp. : 932-952

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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.

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