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Synthesis and anti-proliferative activity of allogibberic acid derivatives containing 1,2,3-triazole pharmacophore
Wu, Ming-Jiang; Wu, Dong-Mei; Chen, Jing-Bo; Zhao, Jing-Feng; Gong, Liang; Gong, Ya-Xiao; Li, Yan; Yang, Xiao-Dong; Zhang, Hongbin
2018
Source PublicationBIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN0960-894X
Volume28Issue:14Pages:2543-2549
AbstractSixty novel allogibberic acid derivatives containing 1,2,3-triazole pharmacophore were designed and synthesized. The key chemical processes include aromatization of the A ring in gibberellins, formation of allogibberic azides and its copper mediated Huisgen 1,3-dipolar cycloaddition with alkynes. A number of hybrids containing a, ss-unsaturated ketone moiety exhibited excellent in vitro cytotoxic activities. Some of the hybrids were more selective to MCF-7 and SW480 cell lines with IC50 values at least 8-fold more cytotoxic than cisplatin (DDP). The most potent compounds C43 and C45 are more cytotoxic than cisplatin (DDP) against all tested five tumor cell lines, with IC50 values of 0.25-1.72 mu M. Mechanism of action studies indicated that allogibberic-triazole derivative C45 could induce the S phase cell cycle arrest and apoptosis in SMMC-7721 cell lines.
Indexed BySCI
Language英语
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/64704
Collection中国科学院昆明植物研究所
Recommended Citation
GB/T 7714
Wu, Ming-Jiang,Wu, Dong-Mei,Chen, Jing-Bo,et al. Synthesis and anti-proliferative activity of allogibberic acid derivatives containing 1,2,3-triazole pharmacophore[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2018,28(14):2543-2549.
APA Wu, Ming-Jiang.,Wu, Dong-Mei.,Chen, Jing-Bo.,Zhao, Jing-Feng.,Gong, Liang.,...&Zhang, Hongbin.(2018).Synthesis and anti-proliferative activity of allogibberic acid derivatives containing 1,2,3-triazole pharmacophore.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,28(14),2543-2549.
MLA Wu, Ming-Jiang,et al."Synthesis and anti-proliferative activity of allogibberic acid derivatives containing 1,2,3-triazole pharmacophore".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 28.14(2018):2543-2549.
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