The Development of Tyrosyl-DNA Phosphodiesterase 1 Inhibitors. Combination of Monoterpene and Adamantine Moieties via Amide or Thioamide Bridges

The Development of Tyrosyl-DNA Phosphodiesterase 1 Inhibitors. Combination of Monoterpene and Adamantine Moieties via Amide or Thioamide Bridges

Eleven amide and thioamide derivatives with monoterpene and adamantine substituents were synthesised. They were tested for their activity against the tyrosyl-DNA phosphodiesterase 1 DNA (Tdp1) repair enzyme with the most potent compound <b>47a</b>, having an IC<sub>50</sub> v...

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Bibliographic Details
Main Authors: Arina A. Chepanova, Evgenii S. Mozhaitsev, Aldar A. Munkuev, Evgeniy V. Suslov, Dina V. Korchagina, Olga D. Zakharova, Alexandra L. Zakharenko, Jinal Patel, Daniel M. Ayine-Tora, Jóhannes Reynisson, Ivanhoe K. H. Leung, Konstantin P. Volcho, Nariman F. Salakhutdinov, Olga I. Lavrik
Format: Article
Language:English
Published: MDPI AG 2019-07-01
Series:Applied Sciences
Subjects:
topotecan
A-549 lung adenocarcinoma cell line l
Topoisomerase 1
molecular modelling
chemical space
synergy
thermal shift assay
intrinsic tryptophan fluorescence binding assay
fluorescence biosensor assay
Online Access:https://www.mdpi.com/2076-3417/9/13/2767

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https://www.mdpi.com/2076-3417/9/13/2767

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