A Novel Class of Tyrosyl-DNA Phosphodiesterase 1 Inhibitors That Contains the Octahydro-2H-chromen-4-ol Scaffold

• Published in: Molecules (Basel, Switzerland) Vol. 23; no. 10; p. 2468
• Main Authors: Li-Zhulanov, Nikolai S., Zakharenko, Alexandra L., Chepanova, Arina A., Patel, Jinal, Zafar, Ayesha, Volcho, Konstantin P., Salakhutdinov, Nariman F., Reynisson, Jóhannes, Leung, Ivanhoe K. H., Lavrik, Olga I.
• Format: Journal Article
• Language: English
• Published: MDPI 26.09.2018; MDPI AG
• Subjects: anticancer agent; biochemical assay; chemical space; DNA repair enzyme; molecular modeling; structural-activity relationships; synthesis; Tdp1 inhibitor

Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is a DNA repair enzyme that mends topoisomerase 1-mediated DNA damage. Tdp1 is a current inhibition target for the development of improved anticancer treatments, as its inhibition may enhance the therapeutic effect of topoisomerase 1 poisons. Here, we report a...