A Novel Synthetic Route for Lysine‐Specific Demethylase 1‐Targeting Compounds: CC‐90011 and MS9117
Abstract
Lysine‐specific demethylase 1 (LSD1) is a crucial target due to its essential role in cancers. CC‐90011 , the reversible and highly selective LSD1 inhibitor at the clinical stage, has demonstrated significant therapeutic potential in acute myeloid leukemia and solid tumors. Herein, we present a novel synthetic route to LSD1‐targeting compounds that enables late‐stage diversification; the key intermediate LYY‐23 was used to synthesize CC‐90011 and MS9117 . In addition, compounds LYY‐25 ∼ LYY‐29 were synthesized and evaluated for LSD1 inhibition, all of which showed inhibitory activity, with LYY‐28 emerging as the most potent compound (IC 50 = 3.59 nM).
Fields of Study & Subjects
Heterocyclic Compound Synthesis and Bioactivity
Epigenetics and DNA Methylation
Protein Degradation and Inhibitors
Publication details
- Journal / source
- ChemMedChem
- Volume
- 21
- Issue
- 5
- Pages
- e202501081–e202501081
- Publication date
- 3 March 2026
- Language
- EN