Novel 2-aryl-4-(4′-hydroxyphenyl)-5H-indeno[1,2-b]pyridines as potent DNA non-intercalative topoisomerase catalytic inhibitors

详细信息    查看全文

• 作者：Seojeong Park^a ; ¹ ; Tara Man Kadayat^b ; ¹ ; Kyu-Yeon Jun^a ; Til Bahadur Thapa Magar^b ; Ganesh Bist^b ; Aarajana Shrestha^b ; Eung-Seok Lee^b ; ^{eslee@yu.ac.kr} ; Youngjoo Kwon^a ; ^{ykwon@ewha.ac.kr}
• 关键词：Anticancer agents ; 2-Aryl-4-(4&prime ; -hydroxyphenyl)-5H-indeno[1 ; 2-b]pyridine ; Antiproliferative activity ; Docking study ; Dual topoisomerase I and II inhibitors
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：14-28
• 全文大小：1512 K
• 卷排序：125

文摘

A new series of rigid 2-aryl-4-(4′-hydroxyphenyl)-5H-indeno[1,2-b]pyridines were synthesized. Compound 16 inhibited most strongly both topo I and topo IIα and cell proliferation. The mode of action of compound 16 was determined to be DNA non-intercalative topo catalytic inhibitor. Molecular docking study suggested that compound 16 inhibited both topo I and topo IIα.