[HTML][HTML] Metabolic profiles of new unsymmetrical bisacridine antitumor agents in electrochemical and enzymatic noncellular systems and in tumor cells

A Mieszkowska, AM Nowicka, A Kowalczyk, A Potęga… - Pharmaceuticals, 2021 - mdpi.com
New unsymmetrical bisacridines (UAs) demonstrated high activity not only against a set of
tumor cell lines but also against human tumor xenografts in nude mice. Representative UA …

[HTML][HTML] Novel insights into conjugation of antitumor-active unsymmetrical bisacridine C-2028 with glutathione: Characteristics of non-enzymatic and glutathione S …

A Potęga, M Kosno, Z Mazerska - Journal of Pharmaceutical Analysis, 2021 - Elsevier
Unsymmetrical bisacridines (UAs) are a novel potent class of antitumor-active therapeutics.
A significant route of phase II drug metabolism is conjugation with glutathione (GSH), which …

Electrochemistry/mass spectrometry (EC/MS) for fast generation and identification of novel reactive metabolites of two unsymmetrical bisacridines with anticancer …

A Potęga, V Göldner, E Niehaves… - … of Pharmaceutical and …, 2023 - Elsevier
The development of a new drug requires knowledge about its metabolic fate in a living
organism, regarding the comprehensive assessment of both drug therapeutic activity and …

Electrochemical simulation of metabolic reduction and conjugation reactions of unsymmetrical bisacridine antitumor agents, C-2028 and C-2053

A Potęga, S Paczkowski, E Paluszkiewicz… - … of Pharmaceutical and …, 2021 - Elsevier
Electrochemistry (EC) coupled with analysis techniques such as liquid chromatography (LC)
and mass spectrometry (MS) has been developed as a powerful tool for drug metabolism …

[HTML][HTML] Acid–base equilibrium and self-association in relation to high antitumor activity of selected unsymmetrical bisacridines established by extensive chemometric …

M Kosno, T Laskowski, JE Frackowiak, A Potęga… - Molecules, 2022 - mdpi.com
Unsymmetrical bisacridines (UAs) represent a novel class of anticancer agents previously
synthesized by our group. Our recent studies have demonstrated their high antitumor …

[HTML][HTML] In Vitro Enzyme Kinetics and NMR-Based Product Elucidation for Glutathione S-Conjugation of the Anticancer Unsymmetrical Bisacridine C-2028 in Liver …

A Potęga, D Rafalska, D Kazimierczyk, M Kosno… - Molecules, 2023 - mdpi.com
This work is the next step in studying the interplay between C-2028 (anticancer-active
unsymmetrical bisacridine developed in our group) and the glutathione S-transferase …

[HTML][HTML] Enhanced activity of P4503A4 and UGT1A10 induced by acridinone derivatives c-1305 and c-1311 in MCF-7 and HCT116 cancer cells: Consequences for …

M Pawłowska, A Kwaśniewska, Z Mazerska… - International Journal of …, 2020 - mdpi.com
Activity modulation of drug metabolism enzymes can change the biotransformation of
chemotherapeutics and cellular responses induced by them. As a result, drug-drug …

Modulation of UDP-glucuronidation by acridinone antitumor agents C-1305 and C-1311 in HepG2 and HT29 cell lines, despite slight impact in noncellular systems

A Bejrowska, M Pawłowska, A Mróz… - Pharmacological Reports, 2018 - Elsevier
Background Among the studied antitumor acridinone derivatives developed in our
laboratory, 5-dimethylaminopropylamino-8-hydroxytriazoloacridinone (C-1305) and 5 …

[HTML][HTML] Glutathione-mediated conjugation of anticancer drugs: an overview of reaction mechanisms and biological significance for drug detoxification and …

A Potęga - Molecules, 2022 - mdpi.com
The effectiveness of many anticancer drugs depends on the creation of specific metabolites
that may alter their therapeutic or toxic properties. One significant route of biotransformation …

[HTML][HTML] c-Myc protein level affected by unsymmetrical bisacridines influences apoptosis and senescence induced in HCT116 colorectal and H460 lung cancer cells

M Pawłowska, J Kulesza, E Augustin - International Journal of Molecular …, 2022 - mdpi.com
Unsymmetrical bisacridines (UAs) are highly active antitumor compounds. They contain in
their structure the drugs previously synthesized in our Department: C-1311 and C-1748. UAs …