Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 56, Issue 6, Pages 2695-2699Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm301782e
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Funding
- Warren family
- Grant NIH/MLPCN [U54 MH084659]
- Predoctoral ACS Medicinal Chemistry Fellowship
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An iterative parallel synthesis effort identified a PLD2 selective inhibitor, ML298 (PLD1 IC50 > 20 000 nM, PLD2 IC50 = 355 nM) and a dual PLD1/2 inhibitor, ML299 (PLD1 IC50 = 6 nM, PLD2 IC50 = 20 nM). SAR studies revealed that a small structural change (incorporation of a methyl group) increased PLD1 activity within this classically PLD2-preferring core and that the effect was enantiospecific. Both probes decreased invasive migration in U87-MG glioblastoma cells.
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