Abstract
We have identified the N(1)-benzyl-N(2)-methylethane-1,2-diamine unit as a substitute for the (S)-alanine benzylamide moiety for the design of co-activator associated arginine methyltransferase 1 (CARM1) inhibitors. The potency of these inhibitors is in the same order of magnitude as their predecessors and their clearance, volume of distribution, and half lives were greatly improved.
MeSH terms
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Diamines / chemical synthesis
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Diamines / chemistry
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Diamines / pharmacology*
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Drug Design
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Models, Molecular
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Molecular Structure
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Protein-Arginine N-Methyltransferases / antagonists & inhibitors*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Diamines
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Enzyme Inhibitors
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Protein-Arginine N-Methyltransferases
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coactivator-associated arginine methyltransferase 1