SYNTHESIS OF LSD1 INHIBITOR-PYRROLEIMIDAZQLE POLYAMIDE CONJUGATES FOR REGION-SPECIFIC ALTERATIONS OF HISTONE MODIFICATION

摘要

Synthetic method of LSD1 inhibitor-pyrrole-imidazole poly amide conjugates for region-specific alterations of histone modification is described. A (1S,2R)-tranylcypromine (PCPA) unit was coupled with an L-lysine part using a nosyl strategy. Conjugation of the inhibitor part with PIP tetramer units was achieved by amide bond formation using PyBOP as a condensation reagent.