Synthesis and biological activity of ferrocenyl indeno[1,2-c]isoquinolines as topoisomerase II inhibitors

详细信息    查看全文

• 作者：Nathalie Wambang^a ; ^b ; Nadè ; ge Schifano-Faux^c ; Alexandre Aillerie^a ; Brigitte Baldeyrou^d ; Camille Jacquet^a ; Christine Bal-Mahieu^d ; Till Bousquet^a ; ^{till.bousquet@univ-lille1.fr" class="auth_mail" title="E-mail the corresponding author} ; Sylvain Pellegrini^a ; Peter T. Ndifon^b ; Samuel Meignan^d ; Jean-Franç ; ois Goossens^c ; Amé ; lie Lansiaux^e ; Lydie Pé ; linski^a ; ^{lydie.pelinski@univ-lille1.fr" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Indenoisoquinoline ; Ferrocene ; Topoisomerase II inhibitor ; Drug binding ; Cytotoxicity
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2016
• 出版时间：15 February 2016
• 年：2016
• 卷：24
• 期：4
• 页码：651-660
• 全文大小：1100 K

文摘

Three series of indeno[1,2-c]isoquinolines bearing a ferrocenyl entity were synthesized and evaluated for DNA interaction, topoisomerase I and II inhibition, and cytotoxicity against breast human cancer cell lines. In the first and second series, the ferrocenyl scaffold was inserted as a linker between the two nitrogen atoms. In the last series, it was introduced at the end of the carbon chain. The present study showed that the ferrocenyl entity enhanced the topoisomerase II inhibition. Most compounds showed a potent growth inhibitory effect on MDA-MB-231 cell line with the IC₅₀ in μM range.