Synthesis and in vitro evaluation of pyrimidine-fused 3-alkenyloxindoles as potential anticancer agents

doi:10.1016/j.tetlet.2016.07.100

	Synthesis and in vitro evaluation of pyrimidine-fused 3-alkenyloxindoles as potential anticancer agents
	Liu, Xiong-Li; Feng, Ting-Ting; Wang, Dan-Dan; Liu, Huan-Huan; Yang, Chao; Li, Xiao-Nian; Lin, Bing; Zhao, Zhi; Zhou, Ying
	2016-09-07
发表期刊	TETRAHEDRON LETTERS
卷号	57 期号:36 页码:4113-4118
摘要	Developed herein was an expedient method toward the synthesis of pyrimidine-fused 3-alkenyloxindoles 4 via a Knoevenagel condensation/SNAr sequential reaction of pyrimidine aldehydes 1 with 2-oxindoles 2 using alcohols 3 as both the solvents and the reactants. A wide variety of products, which is a typical hybridization of two key structural skeletons of 3-alkenyl-oxindole and pyrimidine found in an array of biologically active natural products and pharmaceutical compounds, were obtained smoothly with high efficiency (up to 93% yield) and high (E/Z)-selectivities (up to >20:1 E/Z). Furthermore, their biological activity has been preliminarily demonstrated by in vitro evaluation against human prostate cancer cells PC-3, human lung cancer cells A549 and human leukemia cells K562 by the MTT-based assays using the commercially available broad-spectrum anticancer drug Cisplatin as a positive control. These results suggested that most of pyrimidine-fused 3-alkenyloxindoles 4 showed equipotent or more potent than the positive control of Cisplatin (up to 5.1 times), which suggested that pyrimidine-fused 3-alkenyloxindoles 4 may be potential leads for further biological screenings. (C) 2016 Elsevier Ltd. All rights reserved.
关键词	Knoevenagel Condensation Snar Reaction Molecular Hybridization Pyrimidine-fused 3-alkenyloxindoles Antitumor Activity
DOI	10.1016/j.tetlet.2016.07.100
收录类别	SCI
语种	英语
WOS记录号	WOS:000382338200033
引用统计
文献类型	期刊论文
条目标识符	http://ir.kib.ac.cn/handle/151853/28606
专题	植物化学与西部植物资源持续利用国家重点实验室
推荐引用方式 GB/T 7714	Liu, Xiong-Li,Feng, Ting-Ting,Wang, Dan-Dan,et al. Synthesis and in vitro evaluation of pyrimidine-fused 3-alkenyloxindoles as potential anticancer agents[J]. TETRAHEDRON LETTERS,2016,57(36):4113-4118.
APA	Liu, Xiong-Li.,Feng, Ting-Ting.,Wang, Dan-Dan.,Liu, Huan-Huan.,Yang, Chao.,...&Zhou, Ying.(2016).Synthesis and in vitro evaluation of pyrimidine-fused 3-alkenyloxindoles as potential anticancer agents.TETRAHEDRON LETTERS,57(36),4113-4118.
MLA	Liu, Xiong-Li,et al."Synthesis and in vitro evaluation of pyrimidine-fused 3-alkenyloxindoles as potential anticancer agents".TETRAHEDRON LETTERS 57.36(2016):4113-4118.

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