2-Chlorophenyl-substituted benzofuro[3, 2-b]pyridines with enhanced topoisomerase inhibitory activity: The role of the chlorine substituent. Issue 15 (1st August 2017)

• Record Type: Journal Article
• Authors: Thapa Magar, Til Bahadur; Kadayat, Tara Man; Lee, Hwa-Jong; Park, Seojeong; Bist, Ganesh; Shrestha, Aarajana; Kwon, Youngjoo; Lee, Eung-Seok
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 15(2017)
• Page Start: 3279
• Page End: 3283
• Publication Date: 2017-08-01
• Subjects: Heterocycles -- Benzofuro[3, 2-b]pyridines -- Chlorine-substituent -- Topoisomerase I and II inhibition -- Antiproliferative activity; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.06.025
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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. Compounds17 –19, 23, 24, 26, and27 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.