Michelle Armstrong
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Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity.

Lewis JA, Scott SA, Lavieri R, Buck JR, Selvy PE, Stoops SL, Armstrong MD, Brown HA, Lindsley CW
Bioorg Med Chem Lett. 2009 19 (7): 1916-20

PMID: 19268584 · PMCID: PMC3791604 · DOI:10.1016/j.bmcl.2009.02.057

This Letter describes the synthesis and structure-activity-relationships (SAR) of isoform-selective PLD inhibitors. By virtue of the installation of alternative halogenated piperidinyl benzimidazolone privileged structures, in combination with a key (S)-methyl group, novel PLD inhibitors with low nM potency and unprecedented levels of PLD1 isoform selectivity (approximately 1700-fold) over PLD2 were developed.

MeSH Terms (11)

Benzimidazoles Cell Line Domperidone Drug Design Enzyme Inhibitors Halogenation Humans Phospholipase D Protein Isoforms Structure-Activity Relationship Substrate Specificity

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