- Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity.
Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity.
Bioorganic & medicinal chemistry letters (2009-03-10)
Jana A Lewis, Sarah A Scott, Robert Lavieri, Jason R Buck, Paige E Selvy, Sydney L Stoops, Michelle D Armstrong, H Alex Brown, Craig W Lindsley
PMID19268584
ABSTRACT
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.
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