Novel Tdp1 Inhibitors Based on Adamantane Connected with Monoterpene Moieties via Heterocyclic Fragments

• Published in: Molecules (Basel, Switzerland) Vol. 26; no. 11; p. 3128
• Main Authors: Munkuev, Aldar A., Mozhaitsev, Evgenii S., Chepanova, Arina A., Suslov, Evgeniy V., Korchagina, Dina V., Zakharova, Olga D., Ilina, Ekaterina S., Dyrkheeva, Nadezhda S., Zakharenko, Alexandra L., Reynisson, Jóhannes, Volcho, Konstantin P., Salakhutdinov, Nariman F., Lavrik, Olga I.
• Format: Journal Article
• Language: English
• Published: Basel MDPI AG 24.05.2021; MDPI
• Subjects: Antifungal agents; Apoptosis; cancer; Cancer therapies; Cytotoxicity; DNA repair; DNA repair enzyme; molecular modeling; monoterpenoid; Physicochemical properties; Reagents; SAR; topoisomerase 1

Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is a promising target for anticancer therapy due to its ability to counter the effects topoisomerase 1 (Top1) poison, such as topotecan, thus, decreasing their efficacy. Compounds containing adamantane and monoterpenoid residues connected via 1,2,4-triazole or...