DSpace at EWHA: 2-Chlorophenyl-substituted benzofuro[3,2-b]pyridines with enhanced topoisomerase inhibitory activity: The role of the chlorine substituent

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2-Chlorophenyl-substituted benzofuro[3,2-b]pyridines with enhanced topoisomerase inhibitory activity: The role of the chlorine substituent

Title: 2-Chlorophenyl-substituted benzofuro[3,2-b]pyridines with enhanced topoisomerase inhibitory activity: The role of the chlorine substituent

Authors: Thapa Magar T.B.; Kadayat T.M.; Lee H.-J.; Park S.; Bist G.; Shrestha A.; Kwon Y.; Lee E.-S.

Citation: Bioorganic and Medicinal Chemistry Letters vol. 27, no. 15, pp. 3279 - 3283

Keywords: Antiproliferative activity; Benzofuro[3,2-b]pyridines; Chlorine-substituent; Heterocycles; Topoisomerase I and II inhibition

Abstract: A new series of 2-chloropheny-substituted benzofuro[3,2-b]pyridines were designed, synthesized, and evaluated for topoisomerase I and II inhibition and antiproliferative activity. Compounds 17–19, 23, 24, 26, and 27 exhibited excellent topo II inhibitory activity. A systematic structure-activity relationship study revealed the important role of chlorine substitution in the strong topoisomerase inhibitory activity. © 2017 Elsevier Ltd