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Abstract
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.
Highlights
Furo[3,2-c]pyridines belong to a novel class of heterocycles that exhibit a wide range of biological activities [1,2,3]
Upon a thorough condition screening, the formation of 2a could not be observed at all [Supplementary materials]
Condition screening, the formation of 2a could not be observed at all [supplementary materials]
Summary
Furo[3,2-c]pyridines belong to a novel class of heterocycles that exhibit a wide range of biological activities [1,2,3]. A large number of heterocyclic compounds bearing a furo[3,2-c]pyridine core have been reported as anticancer (Figure 1A, compounds A and B) [4,5] or antibacterial agents (Figure 1A, compound C) [6]. The tricyclic furo[3,2-c]quinoline skeleton possessing a fused aryl ring on the pyridine part has shown unique pharmaceutical and biological activities. Agrawal et al reported that compound F may be a potential topoisomerase-II inhibitor based on related computational studies [9]. In view of the diverse biological activities of such molecules, the design and synthesis of novel heterocyclic structures possessing the furo[3,2-c]pyridine skeleton would be highly valuable for biological studies. As our continuous research interest, we design and synthesize a new type of tetracyclic benzofuro[3,2-c]quinoline (Figure 1B, compound G) that contains
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