Synthesis and anti-proliferative activity of allogibberic acid derivatives containing 1,2,3-triazole pharmacophore

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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 Publication	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN	0960-894X
Volume	28 Issue:14 Pages:2543-2549
Abstract	Sixty 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 By	SCI
Language	英语
Document Type	期刊论文
Identifier	http://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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