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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

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

Matthew C O'Reilly, Sarah A Scott, Kyle A Brown, Thomas H Oguin 3rd, Paul G Thomas, J Scott Daniels, Ryan Morrison, H Alex Brown, Craig W Lindsley

J Med Chem. 2013 Mar 28;56(6):2695-9.

PMID: 23445448

Abstract:

An iterative parallel synthesis effort identified a PLD2 selective inhibitor, ML298 (PLD1 IC50 > 20000 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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1426916020	ML298		1426916-02-0	Price

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