Synthesis, structure-activity relationships and biological evaluation of 7-phenyl-pyrroloquinolinone 3-amide derivatives as potent antimitotic agents

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• 作者：Davide Carta^a ; Roberta Bortolozzi^b ; Mattia Sturlese^a ; Veronica Salmaso^a ; Ernest Hamel^c ; Giuseppe Basso^b ; Laura Calderan^a ; Luigi Quintieri^a ; Stefano Moro^a ; Giampietro Viola^b ; Maria Grazia Ferlin^a ; ^{mariagrazia.ferlin@unipd.it}
• 关键词：Microtubules ; Phenylpyrroloquinolinone ; Tubulin ; Apoptosis ; Molecular docking ; Structure-activity relationships
• 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：643-660
• 全文大小：1970 K
• 卷排序：127

文摘

A small library of 7-pyrrolo[3,2-f]quinolinones was synthesized. The most active compound 4a showed GI50s ranging from 0.1 to 16 nM. Compound 4a did not induce significant cell death in normal human lymphocytes. Compounds, 4a strongly inhibited tubulin assembly assay with an IC50 of 0.89 μM. Compound 4a induce apoptosis through the mitochondrial pathway.