Click chemistry-based synthesis and cytotoxic activity evaluation of 4 alpha-triazole acetate podophyllotoxin derivatives

doi:10.1111/cbdd.13436

KMS > 免疫化学研究所 > 特聘教授组 > Richard A. Lerner组

	Click chemistry-based synthesis and cytotoxic activity evaluation of 4 alpha-triazole acetate podophyllotoxin derivatives
	Hou, Wei 1; Zhang, Guanjun 2; Luo, Zhi 3; Su, Lin 1; Xu, Hongtao4
	2019-04
发表期刊	CHEMICAL BIOLOGY & DRUG DESIGN
ISSN	1747-0277
卷号	93 期号:4 页码:473-483
发表状态	已发表
DOI	10.1111/cbdd.13436
摘要	A series of novel 4 alpha-triazole acetate podophyllotoxin derivatives were synthesized via click chemistry. In vitro cytotoxic activity evaluation showed that most of the derivatives exhibited potent inhibitory activities against the tested cancer cell lines with low nanomolar IC50 values. Further studies demonstrated that compound 31 exhibited broad-spectrum cytotoxic activities, effectively overcame drug-resistance, and showed relatively weak cytotoxicity on non-cancer cells. Preliminary mechanistic studies indicated that 31 might have action on microtubule, cause cell cycle arrest at G(2)/M phase, and induce apoptosis in human PC-3 cancer cells.
关键词	apoptosis click chemistry drug-resistance G(2) M phase podophyllotoxin
收录类别	SCI ; SCIE ; IC
语种	英语
资助项目	Zhejiang University of Technology, China[2017116002229]
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
WOS类目	Biochemistry & Molecular Biology ; Chemistry, Medicinal
WOS记录号	WOS:000462929000009
出版者	WILEY
WOS关键词	ABIETANE DITERPENOID LIBRARY ; BIOLOGICAL EVALUATION ; ANTITUMOR-ACTIVITY ; NATURAL-PRODUCTS ; MULTIDRUG-RESISTANCE ; D-RING ; ANTICANCER ; DESIGN ; CANCER ; POTENT
原始文献类型	Article
引用统计
文献类型	期刊论文
条目标识符	https://kms.shanghaitech.edu.cn/handle/2MSLDSTB/34252
专题	免疫化学研究所_特聘教授组_抗体设计学实验室
通讯作者	Su, Lin; Xu, Hongtao
作者单位	1.Zhejiang Univ Technol, Coll Pharmaceut Sci, IDD&CB, Hangzhou, Zhejiang, Peoples R China 2.Tianjin Univ Sci & Technol, Coll Chem Engn & Mat Sci, Tianjin, Peoples R China 3.Shanghai Evergene Biotech Co Ltd, Shanghai, Peoples R China 4.ShanghaiTech Univ, Shanghai Inst Adv Immunochem Studies, Shanghai, Peoples R China
通讯作者单位	免疫化学研究所
推荐引用方式 GB/T 7714	Hou, Wei,Zhang, Guanjun,Luo, Zhi,et al. Click chemistry-based synthesis and cytotoxic activity evaluation of 4 alpha-triazole acetate podophyllotoxin derivatives[J]. CHEMICAL BIOLOGY & DRUG DESIGN,2019,93(4):473-483.
APA	Hou, Wei,Zhang, Guanjun,Luo, Zhi,Su, Lin,&Xu, Hongtao.(2019).Click chemistry-based synthesis and cytotoxic activity evaluation of 4 alpha-triazole acetate podophyllotoxin derivatives.CHEMICAL BIOLOGY & DRUG DESIGN,93(4),473-483.
MLA	Hou, Wei,et al."Click chemistry-based synthesis and cytotoxic activity evaluation of 4 alpha-triazole acetate podophyllotoxin derivatives".CHEMICAL BIOLOGY & DRUG DESIGN 93.4(2019):473-483.