Design, Synthesis, and In Vitro Evaluation of Benzofuro[3,2-<i>c</i>]Quinoline Derivatives as Potential Antileukemia Agents
Ying Lin,
Dong Xing,
Wen-Biao Wu,
Gao-Ya Xu,
Li-Fang Yu,
Jie Tang,
Yu-Bo Zhou,
Jia Li,
Fan Yang
Affiliations
Ying Lin
Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200062, China
Dong Xing
Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200062, China
Wen-Biao Wu
National Center for Drug Screening, Shanghai Institute of Material Medica, Chinese Academy of Science, Shanghai 201203, China
Gao-Ya Xu
National Center for Drug Screening, Shanghai Institute of Material Medica, Chinese Academy of Science, Shanghai 201203, China
Li-Fang Yu
Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200062, China
Jie Tang
Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200062, China
Yu-Bo Zhou
National Center for Drug Screening, Shanghai Institute of Material Medica, Chinese Academy of Science, Shanghai 201203, China
Jia Li
National Center for Drug Screening, Shanghai Institute of Material Medica, Chinese Academy of Science, Shanghai 201203, China
Fan Yang
Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200062, China
Herein, we design and synthesize an array of benzofuro[3,2-c]quinolines starting from 3-(2-methoxyphenyl)quinolin-4(1H)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-c]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.
