文献类型：期刊文献

英文题名：Design and synthesis of novel sugar-based nitrogen-containing heterocycles as potential anticancer agents under microwave in water

作者：Liu, Jian[1];Wu, Chunlei[1];Jin, Huimin[1];Du, Kui[1];Zheng, Hui[2]

机构：[1]Shaoxing Univ, Sch Chem & Chem Engn, Shaoxing 312000, Peoples R China;[2]Hangzhou Normal Univ, Coll Mat Chem & Chem Engn, Hangzhou 310016, Zhejiang, Peoples R China

年份：2019

卷号：56

期号：11

起止页码：3088

外文期刊名：JOURNAL OF HETEROCYCLIC CHEMISTRY

收录：SCI-EXPANDED(收录号：WOS:000485077100001)、、Scopus(收录号：2-s2.0-85071774718)、WOS

基金：Public Projects of Zhejiang Province of China, Grant/Award Number: LGG19B02002; Zhejiang Provincial Natural Science Foundation of China, Grant/Award Number: No. Y19B060017 LY19B060007; National Natural Science Foundation of China, Grant/Award Number: 21978061

语种：英文

外文摘要：A series of novel glycosyl nitrogen-containing heterocycles derivatives were designed and synthesized. With the help of microwave, the reaction was carried out in water rapidly and afforded the target compounds in good yields. The acid catalysts that were essential for this kind of reaction under traditional heating method were avoided through this strategy. Preliminary biological evaluation showed that most of the compounds could inhibit the growth of A549 cells, but the inhibition of HepG-2 cells was relatively poor. Notably, compound 2i displayed the best potency with an IC50 value of 3.42 mu M against A549 cell lines, which is comparable with the common anticarcinogen paclitaxel (5.12 mu M). Molecular modeling studies suggested that 2i may bind to the ATP-binding site of epidermal growth factor receptor (EGFR), indicating a rational design strategy. These results provide a starting point for designing glycosyl nitrogen-containing heterocycles as the potential drugs in lung cancer therapy.