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

doi:10.3390/molecules25010203

Molecules (Jan 2020)

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

DOI: https://doi.org/10.3390/molecules25010203
Journal volume & issue: Vol. 25, no. 1
p. 203

Abstract

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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.

Published in Molecules

ISSN: 1420-3049 (Online)
Publisher: MDPI AG
Country of publisher: Switzerland
LCC subjects: Science: Chemistry: Organic chemistry
Website: http://www.mdpi.com/journal/molecules

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