Novel Inhibitors of DNA Repair Enzyme TDP1 Combining Monoterpenoid and Adamantane Fragments

• Published in: Anti-cancer agents in medicinal chemistry Vol. 19; no. 4; p. 463
• Main Authors: Mozhaitsev, Evgenii S, Zakharenko, Alexandra L, Suslov, Evgeniy V, Korchagina, Dina V, Zakharova, Olga D, Vasil'eva, Inna A, Chepanova, Arina A, Black, Ellena, Patel, Jinal, Chand, Raina, Reynisson, Jóhannes, Leung, Ivanhoe K H, Volcho, Konstantin P, Salakhutdinov, Nariman F, Lavrik, Olga I
• Format: Journal Article
• Language: English
• Published: Netherlands 01.01.2019
• Subjects: Adamantane - analysis; Catalytic Domain; Cell Line, Tumor; DNA Repair; Drug Screening Assays, Antitumor; Humans; Models, Molecular; Monoterpenes - analysis; Phosphodiesterase Inhibitors - chemistry; Phosphodiesterase Inhibitors - pharmacology; Phosphoric Diester Hydrolases - chemistry; Phosphoric Diester Hydrolases - drug effects; Phosphoric Diester Hydrolases - metabolism; Spectrum Analysis - methods; 3,7-dimethyloctanol; inhibitors; Citronellol; esters; molecular modelling; terpene; chemical space; cytotoxicity

The DNA repair enzyme tyrosyl-DNA-phosphodiesterase 1 (TDP1) is a current inhibition target to improve the efficacy of cancer chemotherapy. Previous studies showed that compounds combining adamantane and monoterpenoid fragments are active against TDP1 enzyme. This investigation is focused on the syn...