The Development of Tyrosyl-DNA Phosphodyesterase 1 (TDP1) Inhibitors Based on the Amines Combining Aromatic/Heteroaromatic and Monoterpenoid Moieties

摘要

Background: Inhibition of the DNA repair enzyme, tyrosyl-DNA phosphodiesterase 1(TDP1), may increase the efficacy of cancer drugs that cause damage to tumor cell DNA. Among the known TDP1 inhibitors, there arc compounds containing moieties of natural substances, e.g., monoterpenoids. In this work, we synthesized several compounds containing aromatic/heteroaromatic amines and monoterpenoid groups and assessed their TDP1 inhibition potential.