| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374899 | Bioorganic & Medicinal Chemistry Letters | 2009 | 8 Pages |
We have identified the N1-benzyl-N2-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.
Graphical abstractWe have identified the N1-benzyl-N2-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.Figure optionsDownload full-size imageDownload as PowerPoint slide
