Synthesis and evaluation of the anti-proliferative activity of diaryl-3-pyrrolin-2-ones and fused analogs |
| |
Authors: | Patricia Mowery Fernando Banales Mejia Courtney L. Franceschi Maeve H. Kean Deborah O. Kwansare Megan M. Lafferty Namita D. Neerukonda Carly E. Rolph Nathanyal J. Truax Erin T. Pelkey |
| |
Affiliation: | 1. Department of Biology, Hobart and William Smith Colleges, Geneva, NY 14456, USA;2. Department of Chemistry, Hobart and William Smith Colleges, Geneva, NY 14456, USA |
| |
Abstract: | 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. |
| |
Keywords: | Indoles Lactams Anti-cancer MTT |
本文献已被 ScienceDirect 等数据库收录! |