Studies on the synthesis of derivatives of marine-derived bostrycin and their structure-activity relationship against tumor cells.
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.
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.
Hong
H
Chen
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.
Lili
L
Zhong
School of Chemistry and Environment, South China Normal University, 348 West Outer Ring Road, Guangzhou 510006, China.
Yuhua
Y
Long
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.
Jia
J
Li
Guangdong Province Key Laboratory of Functional Molecules in Oceanic Microorganism, Bureau of Education, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou 510080, China.|Department of Microbiology, Zhongshan School of Medicine, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou 510080, China.|Key Laboratory of Tropical Disease Control, Ministry of Education, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou 510080, China.
Jueheng
J
Wu
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.
Lan
0000-0003-2765-4015
L
Liu
Guangdong Province Key Laboratory of Functional Molecules in Oceanic Microorganism, Bureau of Education, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou 510080, China.|Department of Microbiology, Zhongshan School of Medicine, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou 510080, China.|Key Laboratory of Tropical Disease Control, Ministry of Education, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou 510080, China.
Shengping
S
Chen
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.
Yongcheng
Y
Lin
Guangdong Province Key Laboratory of Functional Molecules in Oceanic Microorganism, Bureau of Education, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou 510080, China.|Department of Microbiology, Zhongshan School of Medicine, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou 510080, China.|Key Laboratory of Tropical Disease Control, Ministry of Education, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou 510080, China.
Mengfeng
M
Li
Guangdong Province Key Laboratory of Functional Molecules in Oceanic Microorganism, Bureau of Education, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou 510080, China.|Department of Microbiology, Zhongshan School of Medicine, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou 510080, China.|Key Laboratory of Tropical Disease Control, Ministry of Education, Sun Yat-sen University, 74 Zhongshan Road II, Guangzhou 510080, China.
Xun
X
Zhu
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.
Zhigang
Z
She
D000880:Anthraquinones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D045325:HCT116 Cells; D006801:Humans; D013329:Structure-Activity Relationship; D014118:Toxins, Biological / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
D000880:Anthraquinones; D000970:Antineoplastic Agents; D014118:Toxins, Biological; C034287:bostrycin