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Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives
Liao, Sheng-Rong; Qin, Xiao-Chu; Wang, Zhen; Li, Ding; Xu, Liang; Li, Jin-Sheng; Tu, Zheng-Chao; Liu, Yonghong; Liu, YH (reprint author), Chinese Acad Sci, South China Sea Inst Oceanol, Res Ctr Marine Microbes, CAS Key Lab Trop Marine Bioresources & Ecol,Guang, Guangzhou 510301, Guangdong, Peoples R China.
2016
Source PublicationEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume121Pages:500-509
AbstractA series of novel N-1-monoallylated 2,5-diketopiperazine derivatives were designed, synthesized, and evaluated as cytotoxic agents against eight cancer cell lines by using CCK8 assay. These derivatives were substituted with methoxyphenyl groups at C-6 position, and various long alkyl side chains at C-3-position of the 2,5-diketopiperazine ring. The cytotoxic results showed that 4-methoxyphenyl group was better than 2-methoxyphenyl group as optimal substitutive group, while 3-methoxyphenyl group was not a suitable one. When the number (n value) of the methylene groups for the long alkyl side chain was 3 (compounds 1c and 3c), the derivatives had the strongest cytotoxicities. Compound 3c substituted with 4-methoxyphenyl group and pentylidene side chain exhibited strong activity (IC50 = 0.36-1.9 mu M) against all cancer cell lines, and could obviously induce apoptosis of cancer cell line U937 at 1.0 mu M after 48 h treatment. (C) 2016 Elsevier Masson SAS. All rights reserved.
Department[Liao, Sheng-Rong; Li, Jin-Sheng; Liu, Yonghong] Chinese Acad Sci, South China Sea Inst Oceanol, Res Ctr Marine Microbes, CAS Key Lab Trop Marine Bioresources & Ecol,Guang, Guangzhou 510301, Guangdong, Peoples R China; [Qin, Xiao-Chu; Wang, Zhen; Tu, Zheng-Chao] Chinese Acad Sci, Guangzhou Inst Biomed & Hlth, Lab Mol Engn, Guangzhou 510530, Guangdong, Peoples R China; [Qin, Xiao-Chu; Wang, Zhen; Tu, Zheng-Chao] Chinese Acad Sci, Guangzhou Inst Biomed & Hlth, Lab Nat Prod Synth, Guangzhou 510530, Guangdong, Peoples R China; [Li, Ding] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China; [Xu, Liang] Enantiotech Corp Ltd, Zhongshan Torch Hitech, IndustrialDev Zone, Zhongshan 528437, Peoples R China ; LMB
KeywordLong Alkyl Chain 2 Cytotoxic Activity 5-diketopiperazine Derivatives Apoptosis Lipophilicity
Subject AreaPharmacology & Pharmacy
Document Type期刊论文
Identifierhttp://ir.scsio.ac.cn/handle/344004/15279
Collection中科院海洋生物资源可持续利用重点实验室
Corresponding AuthorLiu, YH (reprint author), Chinese Acad Sci, South China Sea Inst Oceanol, Res Ctr Marine Microbes, CAS Key Lab Trop Marine Bioresources & Ecol,Guang, Guangzhou 510301, Guangdong, Peoples R China.
Recommended Citation
GB/T 7714
Liao, Sheng-Rong,Qin, Xiao-Chu,Wang, Zhen,et al. Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2016,121:500-509.
APA Liao, Sheng-Rong.,Qin, Xiao-Chu.,Wang, Zhen.,Li, Ding.,Xu, Liang.,...&Liu, YH .(2016).Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,121,500-509.
MLA Liao, Sheng-Rong,et al."Design, synthesis and cytotoxic activities of novel 2,5-diketopiperazine derivatives".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 121(2016):500-509.
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