DESIGN, SYNTHESIS, IN VITRO ANTIPROLIFERATIVE ACTIVITY EVALUATION OF 2-ALICANOYLAMIDOTHIOPHENE-3-CARBOXAMIDE DERIVATIVES

doi:10.3987/COM-16-13558

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	DESIGN, SYNTHESIS, IN VITRO ANTIPROLIFERATIVE ACTIVITY EVALUATION OF 2-ALICANOYLAMIDOTHIOPHENE-3-CARBOXAMIDE DERIVATIVES
	Zhang, Jiefeng 1; Guan, Fengjie 1; Qiu, Jiakun 1; Fang, Yanfen 1; Yu, Lifang 1; Li, Jingya3 ; Yang, Fan 1; Zhang, Xiongwen 1; Li, Jia3 ; Tang, Jie 1,2
刊名	HETEROCYCLES
	2016-12-01
卷号	92 期号:12 页码:2145-2165
ISSN号	0385-5414
DOI	10.3987/COM-16-13558
文献子类	Article
英文摘要	A series of 2-alkanoylamidothiophene-3-carboxamide derivatives were synthesized based on the hit compound 1. The anti-proliferative activity of all the compounds in vitro against MGC-803 (stomach) and HCT-116 (colon) cancer cell lines using SRB assays were tested. Several compounds showed improved anti-proliferative activity against MGC-803 and HCT-116. SAR study revealed that chlorine substituent in the 2-acetylamino part was important for anti-proliferative activity. 5a, 11b, 11c and lid were the most potent compounds against MGC-803 (IC(50)s = 2.32-2.95 mu M), and 5a and 11c also showed good anti-proliferative activity against HCT-116 cells (IC(50)s = 3.41-3.75 mu M). In addition, the anti-proliferative activity of llb and lid could be attributed to the apoptosis in HCT116 cells via caspase 3 activation, confirmed by flow cytometry assay and western blot analysis. Meanwhile, lib and lid decreased the mitochondrial membrane potential (MMP) in HCT116 cells.
资助项目	National Key Technology RD Program[2015BAK45B00] ; National Natural Science Foundation of China[81472788] ; National Natural Science Foundation of China[81272463] ; Major State Basic Research Development Program of China[2015CB910400] ; Shanghai Science and Technology Council[14DZ0511800] ; Shanghai Science and Technology Council[14142201200] ; Laboratory of Organic Functional Molecules, Sino-French Institute of ECNU[00000000]
WOS关键词	INFLUENZA-VIRUS POLYMERASE ; CYTOCHROME-C RELEASE ; BIOLOGICAL EVALUATION ; INHIBITORS ; THIOPHENE ; APOPTOSIS ; ANTAGONISTS ; DISCOVERY ; RECEPTOR ; 2-ACYLAMINOTHIOPHENE-3-CARBOXAMIDES
WOS研究方向	Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000394078100003
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/275772]
专题	国家新药筛选中心药物安全性评价中心
通讯作者	Fang, Yanfen; Tang, Jie
作者单位	1.East China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, SCME, Shanghai 200062, Peoples R China; 2.East China Normal Univ, SCME, Shanghai Key Lab Green Chem & Chem Proc, Shanghai 200062, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China;
推荐引用方式 GB/T 7714	Zhang, Jiefeng,Guan, Fengjie,Qiu, Jiakun,et al. DESIGN, SYNTHESIS, IN VITRO ANTIPROLIFERATIVE ACTIVITY EVALUATION OF 2-ALICANOYLAMIDOTHIOPHENE-3-CARBOXAMIDE DERIVATIVES[J]. HETEROCYCLES,2016,92(12):2145-2165.
APA	Zhang, Jiefeng.,Guan, Fengjie.,Qiu, Jiakun.,Fang, Yanfen.,Yu, Lifang.,...&Tang, Jie.(2016).DESIGN, SYNTHESIS, IN VITRO ANTIPROLIFERATIVE ACTIVITY EVALUATION OF 2-ALICANOYLAMIDOTHIOPHENE-3-CARBOXAMIDE DERIVATIVES.HETEROCYCLES,92(12),2145-2165.
MLA	Zhang, Jiefeng,et al."DESIGN, SYNTHESIS, IN VITRO ANTIPROLIFERATIVE ACTIVITY EVALUATION OF 2-ALICANOYLAMIDOTHIOPHENE-3-CARBOXAMIDE DERIVATIVES".HETEROCYCLES 92.12(2016):2145-2165.