Synthesis and evaluation of the anti-proliferative activity of diaryl-3-pyrrolin-2-ones and fused analogs

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• 作者：Patricia Mowery^a ; ^{mowery@hws.edu} ; Fernando Banales Mejia^b ; Courtney L. Franceschi^b ; Maeve H. Kean^b ; Deborah O. Kwansare^b ; Megan M. Lafferty^b ; Namita D. Neerukonda^a ; Carly E. Rolph^a ; ^b ; Nathanyal J. Truax^b ; Erin T. Pelkey^b ; ^{pelkey@hws.edu}
• 关键词：Indoles ; Lactams ; Anti-cancer ; MTT
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 January 2017
• 年：2017
• 卷：27
• 期：2
• 页码：191-195
• 全文大小：994 K
• 卷排序：27

文摘

Analogs containing a central 3-pyrrolin-2-one core with different methoxyphenyl and/or indole substituents were prepared and tested for anti-proliferative activity in U-937 cells. The most efficacious analogs were non-rigid, (non-fused) contained methoxyaryl groups located at the 4-position, and contained either methoxyaryl or indole groups located at the 3-position. Both the number of methoxy groups contained in the substituents and the particular location of the indole rings with respect to the lactam carbonyl had significant affects on anti-proliferative activity. This work provides a framework to better understand structure-activity relationships for inducing anti-proliferative activity in diaryl heterocyclic scaffolds.