147471-10-1Relevant academic research and scientific papers
Synthesis and evaluation of the anti-proliferative activity of diaryl-3-pyrrolin-2-ones and fused analogs
Mowery, Patricia,Banales Mejia, Fernando,Franceschi, Courtney L.,Kean, Maeve H.,Kwansare, Deborah O.,Lafferty, Megan M.,Neerukonda, Namita D.,Rolph, Carly E.,Truax, Nathanyal J.,Pelkey, Erin T.
supporting information, p. 191 - 195 (2016/12/27)
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.
(Imidazolylphenyl)pyrrol-2-one inhibitors of cardiac cAMP phosphodiesterase
Lampe,Chou,Hanna,Di Meo,Erhardt,Hagedorn III,Ingebretsen,Cantor
, p. 1041 - 1047 (2007/10/02)
Seven 3-alkyl-4-aryl-1,5-dihydro-2H-pyrrol-2-ones were prepared as potential inhibitors of cardiac cAMP phosphodiesterase (PDE). The design of these compounds made use of rolipram, a known inhibitor of the brain cAMP PDE isozyme, as a lead structure and w
