Rational design, synthesis, and evaluation of novel 2,4-Chloro- and Hydroxy-Substituted diphenyl Benzofuro[3,2-b]Pyridines: Non-intercalative catalytic topoisomerase I and II dual inhibitor

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• 作者：Seojeong Park^a ; ¹ ; Til Bahadur Thapa Magar^b ; ¹ ; Tara Man Kadayat^b ; Hwa Jong Lee^a ; Ganesh Bist^b ; Aarajana Shrestha^b ; Eung-Seok Lee^b ; ^{eslee@ynu.ac.kr} ; Youngjoo Kwon^a ; ^{ykwon@ewha.ac.kr}
• 关键词：2 ; 4-chloro- and hydroxy-substituted diphenyl benzofuro[3 ; 2-b]pyridines ; Dual topoisomerase I and II inhibition ; Antiproliferative activity ; Non-intercalative catalytic inhibiton ; Anticancer agent
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：318-333
• 全文大小：2412 K
• 卷排序：127

文摘

A new class of dual topo inhibitors, 2,4-substituted diphenyl benzofuro[3,2-b]pyridines were prepared. Observed positive correlation with dual topo inhibition and antiproliferative activity. Benzofuran moiety and phenol on 4-position of central pyridine is crucial for both activity. Compound 14 acts as a non-intercalative catalytic dual topo I and II inhibitor.