188943-73-9Relevant articles and documents
Exploring the physicochemical and antiproliferative properties of biaryl-linked [13]-macrodilactones
Chen, Chengsheng,Bosko, Cristin,McGeough, Catherine P.,McLean, Ryan,Zaino, Angela M.,Kyle Hadden,Peczuh, Mark W.
, (2020)
A macrocyclic motif fosters productive protein-small molecule interactions. There are numerous examples of both natural product and designed, synthetic macrocycles that modulate the immune system, slow microbial infection, or kill eukaryotic cells. Reported here are the synthesis, physicochemical characterization, and antiproliferative activity of a group of [13]-macrodilactones decorated with a pendant biaryl moiety. Biaryl analogs were prepared by Suzuki reactions conducted on a common intermediate that contained a bromophenyl unit alpha to one of the carbonyls of the [13]-macrodilactone. Principal component analysis placed the new compounds in physicochemical context relative to a variety of pharmaceuticals and natural products. Modest inhibition of proliferation was observed in ASZ cells, a murine basal cell carcinoma line. This work underscores the value of an approach toward the identification of bioactive compounds that places the evaluation of physicochemical parameters early in the search process.
Diaryl substituted pyrrolidinones and pyrrolones as 5-HT2C inhibitors: Synthesis and biological evaluation
Micheli, Fabrizio,Pasquarello, Alessandra,Tedesco, Giovanna,Hamprecht, Dieter,Bonanomi, Giorgio,Checchia, Anna,Jaxa-Chamiec, Albert,Damiani, Federica,Davalli, Silvia,Donati, Daniele,Gallotti, Chiara,Petrone, Marcella,Rinaldi, Marilisa,Riley, Graham,Terreni, Silvia,Wood, Martyn
, p. 3906 - 3912 (2008/12/21)
Within the continuous quest for the discovery of novel compounds able to treat anxiety and depression, the generation of a pharmacophore model for 5-HT2C receptor antagonists and the discovery of a new class of potent and selective 5-HT2C
5-AMIDOMETHYL ALPHA, BETHA-SATURATED AND -UNSATURATED 3-ARYL BUTYROLACTONE ANTIBACTERIAL AGENTS
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, (2008/06/13)
The present invention provides for new 5-amidomethyl, alpha , beta -saturated and-unsaturated butyrolactone antibacterial agents of formula I I characterized by 3-aryl substituents that include, for example, indolinyl and phenyl substituted with z