Design, Synthesis, and In Vitro Evaluation of Benzofuro[3,2-<i>c</i>]Quinoline Derivatives as Potential Antileukemia Agents

oleh: Ying Lin, Dong Xing, Wen-Biao Wu, Gao-Ya Xu, Li-Fang Yu, Jie Tang, Yu-Bo Zhou, Jia Li, Fan Yang

Format: Article
Diterbitkan: MDPI AG 2020-01-01

Deskripsi

Herein, we design and synthesize an array of benzofuro[3,2-<i>c</i>]quinolines starting from 3-(2-methoxyphenyl)quinolin-4(1<i>H</i>)ones via a sequential chlorination/demethylation, intramolecular cyclization pathway. This sequential transformation was efficient, conducted under metal-free and mild reaction conditions, and yielded corresponding benzofuro[3,2-<i>c</i>]quinolines in high yields. In vitro biological evaluation indicated that such type of compounds showed excellent antileukemia activity and selectivity, and therefore may offer a promising hit compound for developing antileukemia compounds.