Adamantane-Monoterpenoid Conjugates Linked via Heterocyclic Linkers Enhance the Cytotoxic Effect of Topotecan

• Published in: Molecules (Basel, Switzerland) Vol. 27; no. 11; p. 3374
• Main Authors: Munkuev, Aldar A., Dyrkheeva, Nadezhda S., Kornienko, Tatyana E., Ilina, Ekaterina S., Ivankin, Dmitry I., Suslov, Evgeniy V., Korchagina, Dina V., Gatilov, Yuriy V., Zakharenko, Alexandra L., Malakhova, Anastasia A., Reynisson, Jóhannes, Volcho, Konstantin P., Salakhutdinov, Nariman F., Lavrik, Olga I.
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 24.05.2022; MDPI
• Subjects: 1,2,4-triazole; 1,3,4-thiadiazole; adamantane; Antifungal agents; Biosensors; Cancer therapies; Chemotherapy; Chloride; Colorectal cancer; Cytotoxicity; DNA damage; Enzymes; monoterpene; Sulfur; TDP1 inhibitors; Toxicity; tyrosyl-DNA phosphodiesterase 1; TDP1 inhibitors; adamantane; monoterpene; synergy; 1,2,4-triazole; 1,3,4-thiadiazole; tyrosyl-DNA phosphodiesterase 1

Inhibiting tyrosyl-DNA phosphodiesterase 1 (TDP1) is a promising strategy for increasing the effectiveness of existing antitumor therapy since it can remove the DNA lesions caused by anticancer drugs, which form covalent complexes with topoisomerase 1 (TOP1). Here, new adamantane–monoterpene conjuga...