文献类型：期刊文献

英文题名：Synthesis, characterization and biological activity of 1,3-diazaheteroaromatic derivatives by the ring-opening domino reaction

作者：Li, Shikang[1];Huang, Liliang[1];Chen, Zhuo[2];Zhao, Jiangdong[1];Feng, Huangdi[1]

机构：[1]Shanghai Univ Engn Sci, Coll Chem & Chem Engn, 333 Longteng Rd, Shanghai 201620, Peoples R China;[2]East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, 130 Meilong Rd, Shanghai 200237, Peoples R China

年份：2019

卷号：1196

起止页码：245

外文期刊名：JOURNAL OF MOLECULAR STRUCTURE

收录：;EI(收录号：20192607112824);WOS:【SCI-EXPANDED(收录号:WOS:000487930600024)】；

基金：This work was supported by the Start-up funding (E3-0903-18-01269) and the Postgraduate Innovation Program funding (E3-0903-17-01059) from Shanghai University of Engineering Science, the Natural Science Foundation of Shanghai (15ZR1418800), and the China Postdoctoral Science Foundation (2016M601681).

语种：英文

外文关键词：1,3-Diazaheteroaromatic derivatives; Ring-opening domino reaction; X-ray crystallography

摘要：Synthesis of a series of 1,3-diazaheteroaromatic compounds was accomplished by the ring-opening domino reaction of cyclopropane-1,1-dicarboxylates with heterocyclic compounds. The compounds were characterized by NMR (H-1 and C-13) and mass spectral data. A novel single crystal 4b' was successfully cultivated by adding a handful of Y(NO3)(3) to a light yellow viscous oil 4b and organic solvent. X-ray crystal analysis of 4b' indicated that it crystallized in p-1 space group. Additionally, 12 compounds were screened for their cytotoxic activity against the RS4; 11 leukemia cells and H3122 lung cancer cells. The preliminary biological screening results showed that several compounds could inhibit by more than 50% leukemia cell growth at 50 mu M and/or 10 mu M. (C) 2019 Published by Elsevier B.V.