[HTML][HTML] Promising new inhibitors of tyrosyl-DNA phosphodiesterase I (Tdp 1) combining 4-arylcoumarin and monoterpenoid moieties as components of complex …

TM Khomenko, AL Zakharenko, AA Chepanova… - International Journal of …, 2019 - mdpi.com
Tyrosyl-DNA phosphodiesterase 1 (Tdp1) is an important DNA repair enzyme in humans,
and a current and promising inhibition target for the development of new chemosensitizing …

[HTML][HTML] New 5-Hydroxycoumarin-Based Tyrosyl-DNA Phosphodiesterase I Inhibitors Sensitize Tumor Cell Line to Topotecan

TM Khomenko, AL Zakharenko, TE Kornienko… - International Journal of …, 2023 - mdpi.com
Tyrosyl-DNA-phosphodiesterase 1 (TDP1) is an important enzyme in the DNA repair system.
The ability of the enzyme to repair DNA damage induced by a topoisomerase 1 poison such …

[HTML][HTML] Novel TDP1 inhibitors: disubstituted thiazolidine-2, 4-diones containing monoterpene moieties

DI Ivankin, TE Kornienko, MA Mikhailova… - International Journal of …, 2023 - mdpi.com
Tyrosyl-DNA-phosphodiesterase 1 (TDP1) is a promising target for antitumor therapy; the
use of TDP1 inhibitors with a topoisomerase 1 poison such as topotecan is a potential …

[HTML][HTML] The development of Tyrosyl-DNA phosphodiesterase 1 inhibitors. Combination of monoterpene and adamantine moieties via amide or thioamide bridges

AA Chepanova, ES Mozhaitsev, AA Munkuev… - Applied Sciences, 2019 - mdpi.com
Featured Application Inhibition of Tdp1 has the potential to increase the potency of the
anticancer drugs topotecan and irinotecan, topoisomerase 1 poisons. Furthermore, Tdp1 …

Monoterpene substituted thiazolidin-4-ones as novel TDP1 inhibitors: Synthesis, biological evaluation and docking

DI Ivankin, NS Dyrkheeva, AL Zakharenko… - Bioorganic & Medicinal …, 2022 - Elsevier
Abstract Tyrosyl-DNA phosphodiesterase 1 (TDP1) is a promising target for a new therapy in
oncological disease as an adjunct to topoisomerase 1 (TOP1) drugs. In this paper, novel …

[HTML][HTML] New deoxycholic acid derived tyrosyl-DNA phosphodiesterase 1 inhibitors also inhibit tyrosyl-DNA phosphodiesterase 2

OV Salomatina, NS Dyrkheeva, II Popadyuk… - Molecules, 2021 - mdpi.com
A series of deoxycholic acid (DCA) amides containing benzyl ether groups on the steroid
core were tested against the tyrosyl-DNA phosphodiesterase 1 (TDP1) and 2 (TDP2) …

[HTML][HTML] Natural products and their derivatives as inhibitors of the DNA repair enzyme tyrosyl-DNA phosphodiesterase 1

AL Zakharenko, OA Luzina, AA Chepanova… - International Journal of …, 2023 - mdpi.com
Tyrosyl-DNA phosphodiesterase 1 (TDP1) is an important repair enzyme that removes
various covalent adducts from the 3′ end of DNA. Particularly, covalent complexes of …

New fluorescence-based high-throughput screening assay for small molecule inhibitors of tyrosyl-DNA phosphodiesterase 2 (TDP2)

CJA Ribeiro, J Kankanala, K Shi, K Kurahashi… - European Journal of …, 2018 - Elsevier
Abstract Tyrosyl-DNA phosphodiesterase 2 (TDP2) repairs topoisomerase II (TOP2)
mediated DNA damages and causes resistance to TOP2-targeted cancer therapy. Inhibiting …

[HTML][HTML] Novel Tdp1 inhibitors based on adamantane connected with monoterpene moieties via heterocyclic fragments

AA Munkuev, ES Mozhaitsev, AA Chepanova… - Molecules, 2021 - mdpi.com
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 …

5-Arylidenethioxothiazolidinones as inhibitors of tyrosyl–DNA phosphodiesterase I

VR Sirivolu, SKV Vernekar, C Marchand… - Journal of medicinal …, 2012 - ACS Publications
Tyrosyl–DNA phosphodiesterase I (Tdp1) is a cellular enzyme that repairs the irreversible
topoisomerase I (Top1)–DNA complexes and confers chemotherapeutic resistance to Top1 …