2-(1-piperidinylmethyl)phenol and Neoplasms

A recently proposed strategy to overcome multidrug resistance (MDR) in cancer is to target the collateral sensitivity of otherwise resistant cells. We designed a library of 120 compounds to explore the chemical space around previously identified 8-hydroxyquinoline-derived Mannich bases with robust MDR-selective toxicity. We included compounds to study the effect of halogen and alkoxymethyl substitutions in R5 in combination with different Mannich bases in R7, a shift of the Mannich base from R7 to R5, as well as the introduction of an aromatic moiety. Cytotoxicity tests performed on a panel of parental and MDR cells highlight a strong influence of experimentally determined p

Topics: Antineoplastic Agents; Chelating Agents; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Humans; Mannich Bases; Neoplasms; Oxyquinoline; Structure-Activity Relationship