Development of Dual PLD1/2 and PLD2 Selective Inhibitors From a Common 1,3,8-Triazaspiro[4.5]decane Core: Discovery of ML298 and ML299 that Decrease Invasive Migration in U87-MG Glioblastoma Cells

An iterative parallel synthesis effort identified a PLD(2) selective inhibitor, ML298 (PLD(1) IC(50) >20,000 nM, PLD(2) IC(50) = 355 nM) and a dual PLD(1/2) inhibitor, ML299 (PLD(1) IC(50) = 6 nM, PLD(2) IC(50) = 20 nM). SAR studies revealed a small structural change (incorporation of a methyl gr...

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Detalhes bibliográficos
Main Authors: O’Reilly, Matthew C., Scott, Sarah A., Brown, Kyle A., Oguin, Thomas H., Thomas, Paul G., Daniels, J. Scott, Morrison, Ryan, Brown, H. Alex, Lindsley, Craig W.
Formato: Artigo
Idioma:Inglês
Publicado em: 2013
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3632306/
https://ncbi.nlm.nih.gov/pubmed/23445448
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm301782e
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