Výsledky vyhledávání - "Nathalie Derimay"

Preparation and optimization of pyrazolo[1,5-a]pyrimidines as new potent PDE4 inhibitors

Autor: Philippe Chamiot-Clerc, Christelle Mugler, Nathalie Derimay, John Thomas Feutrill, Jacques Le Roux, Frank Halley, Claudine Grepin, Caroline Leriche, David Papin, Laurent Schio

Publikováno v: Bioorganicmedicinal chemistry letters. 26(2)

A new series of pyrazolo[1,5-a]pyrimidines exemplified by compound 1, has been identified with moderate activity (IC50=165nM), following GSK256066 rescaffolding. Compound 1 optimization at positions 2, 3, 6 and 7 gave compound 10 with high in vitro a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d74d975afb98aee33bc583f80731c51
https://pubmed.ncbi.nlm.nih.gov/26681511

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The use of virtual screening and differential scanning fluorimetry for the rapid identification of fragments active against MEK1

Autor: Gary Mccort, Sylvie Llopart, Cyrielle Andouche, François Vallée, Cécile Delorme, Frédéric Foucalt, Maryse Lowinski, Nathalie Derimay, Kwame Amaning, Nis Halland, Antonio Ugolini, Valerie Steier, Alexey Rak, Christophe Marcireau, Stephanie Vougier

Publikováno v: Bioorganicmedicinal chemistry letters. 23(12)

We report the analysis of an in-house fragment screening campaign for the oncology target MEK1. The application of virtual screening (VS) as a primary fragment screening approach, followed by biophysical validation using differential screening fluori

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f721fd74acc7605759c2ba6c5e697493
https://pubmed.ncbi.nlm.nih.gov/23648182

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