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Synthesis, Crystal Structure and Bioactivity of Ethyl 1-((2-Bromophenyl)carbamoyl)-2-(3,4,5-trimethoxyphenyl) cyclopropanecarboxylate
Jia H(贾辉)1; Zhong HY(钟涵宇)2; Zhang JY(张敬一)1
2019
发表期刊结构化学
ISSN0254-5861
卷号38.0期号:012页码:2070-2076
摘要Many small-molecule compounds were reported as microtubule-inhibitor with potential anticancer activities, such as combretastatin-A4(CA-4) analogue. The title compound which is one novel cyclopropylamide analogue of CA-4, namely as ethyl 1-((2-bromophenyl)carbamoyl)-2-(3,4,5-trimethoxyphenyl)cyclopropanecarboxylate, has been synthesized and its crystal structure was characterized by X-ray single-crystal diffraction. The crystal belongs to monoclinic, space group P21/n with a = 8.8002(6), b = 11.4525(8), c = 21.7870(16)A, β = 93.810(3)°, V = 2190.9(3)A^3, Z = 4, C22H23BrNO6, Mr = 477.32, Dc = 1.447 Mg/cm^3, F(000) = 980, λ(Cu Kα) = 1.54178A, μ = 2.883 mm^–1, R = 0.0691 and wR = 0.1958 for 6420 observed reflections(I > 2σ(I)). Importantly, the compound revealed potential anticancer activities in six cancer cells and could stimulate tubulin polymerization in vitro, indicating that the small-molecule could be selected as a lead compound for the development of microtubule stimulator.
关键词cycolpropylamide analogues synthesis bioactivity microtubule-stabilizing agents
收录类别CSCD
语种中文
CSCD记录号CSCD:6631701
引用统计
文献类型期刊论文
条目标识符http://ir.imr.ac.cn/handle/321006/153083
专题中国科学院金属研究所
作者单位1.中国科学院金属研究所
2.Department of Pharmacy,First Affiliated Hospital Medical University
推荐引用方式
GB/T 7714
Jia H,Zhong HY,Zhang JY. Synthesis, Crystal Structure and Bioactivity of Ethyl 1-((2-Bromophenyl)carbamoyl)-2-(3,4,5-trimethoxyphenyl) cyclopropanecarboxylate[J]. 结构化学,2019,38.0(012):2070-2076.
APA 贾辉,钟涵宇,&张敬一.(2019).Synthesis, Crystal Structure and Bioactivity of Ethyl 1-((2-Bromophenyl)carbamoyl)-2-(3,4,5-trimethoxyphenyl) cyclopropanecarboxylate.结构化学,38.0(012),2070-2076.
MLA 贾辉,et al."Synthesis, Crystal Structure and Bioactivity of Ethyl 1-((2-Bromophenyl)carbamoyl)-2-(3,4,5-trimethoxyphenyl) cyclopropanecarboxylate".结构化学 38.0.012(2019):2070-2076.
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