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

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

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...

Full description

Bibliographic Details
Main Authors: Nikolai S. Li-Zhulanov, Alexandra L. Zakharenko, Arina A. Chepanova, Jinal Patel, Ayesha Zafar, Konstantin P. Volcho, Nariman F. Salakhutdinov, Jóhannes Reynisson, Ivanhoe K. H. Leung, Olga I. Lavrik
Format: Article
Language:English
Published: MDPI AG 2018-09-01
Series:Molecules
Subjects:
anticancer agent
Tdp1 inhibitor
DNA repair enzyme
synthesis
biochemical assay
molecular modeling
chemical space
structural-activity relationships
Online Access:http://www.mdpi.com/1420-3049/23/10/2468

Internet

http://www.mdpi.com/1420-3049/23/10/2468

Similar Items