A series of camptothecin prodrugs exhibit HDAC inhibition activity

doi:10.1016/j.bmc.2018.08.008

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	A series of camptothecin prodrugs exhibit HDAC inhibition activity
	Zhu, Qiwen 2; Yu, Xumeng 2; Shen, Qianqian 3; Zhang, Qiumeng 1,2; Su, Mingbo 1; Zhou, Yubo1 ; Li, Jia1 ; Chen, Yi3 ; Lu, Wei 2
刊名	BIOORGANIC & MEDICINAL CHEMISTRY
	2018-09-01
卷号	26 期号:16 页码:4706-4715
关键词	Camptothecin HDAC SAHA Prodrug
ISSN号	0968-0896
DOI	10.1016/j.bmc.2018.08.008
文献子类	Article
英文摘要	Camptothecin plays an important role in clinical cancer treatment, and its derivatives are a favorite of pharmaceutical chemists. Herein, we have designed a series of camptothecin prodrugs that exhibit histone deacetylase (HDAC) inhibition activity based on the synergy effect between HDAC inhibitors and camptothecin derivatives. With the evaluation of stability in buffers or plasma from human or mouse model, an appropriate linker was found, so the active drug can be released efficiently and compound 21a exhibited strong anti-proliferative activity in A549 and HCT-116 cell lines. These results indicated that the well-designed prodrug can be promising in cancer treatment.
资助项目	Shanghai Science and Technology Council[16DZ2280100]
WOS关键词	HISTONE DEACETYLASE INHIBITORS ; CELL LUNG-CANCER ; ANTICANCER DRUGS ; ANTITUMOR AGENTS ; TOPOISOMERASE-I ; COLON-CANCER ; 5-FLUOROURACIL ; COMBINATION ; VORINOSTAT ; EXPRESSION
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000442887900012
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/279599]
专题	药理学第一研究室中科院受体结构与功能重点实验室新药研究国家重点实验室
通讯作者	Chen, Yi; Lu, Wei
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China 2.East China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Sch Chem & Mol Engn, 3663 North Zhongshan Rd, Shanghai 200062, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Div Antitumor Pharmacol, State Key Lab Drug Res, Shanghai 201203, Peoples R China;
推荐引用方式 GB/T 7714	Zhu, Qiwen,Yu, Xumeng,Shen, Qianqian,et al. A series of camptothecin prodrugs exhibit HDAC inhibition activity[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2018,26(16):4706-4715.
APA	Zhu, Qiwen.,Yu, Xumeng.,Shen, Qianqian.,Zhang, Qiumeng.,Su, Mingbo.,...&Lu, Wei.(2018).A series of camptothecin prodrugs exhibit HDAC inhibition activity.BIOORGANIC & MEDICINAL CHEMISTRY,26(16),4706-4715.
MLA	Zhu, Qiwen,et al."A series of camptothecin prodrugs exhibit HDAC inhibition activity".BIOORGANIC & MEDICINAL CHEMISTRY 26.16(2018):4706-4715.