Cu(I) and Cu(II) Complexes Based on Lonidamine-Conjugated Ligands Designed to Promote Synergistic Antitumor Effects

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11320%2F22%3A10457101" target="_blank" >RIV/00216208:11320/22:10457101 - isvavai.cz</a>

Výsledek na webu

<a href="https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=r9nXxV76Pl" target="_blank" >https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=r9nXxV76Pl</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1021/acs.inorgchem.1c03658" target="_blank" >10.1021/acs.inorgchem.1c03658</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Cu(I) and Cu(II) Complexes Based on Lonidamine-Conjugated Ligands Designed to Promote Synergistic Antitumor Effects

Popis výsledku v původním jazyce

Bis(pyrazol-1-yl)- and bis(3,5-dimethylpyrazol-1-yl)-acetates were conjugated with the 2-hydroxyethylester and 2-aminoethylamide derivatives of the antineoplastic drug lonidamine to prepare Cu(I) and Cu(II) complexes that mightact through synergistic mechanisms of action due to the presence of lonidamine and copper in the same chemical entity. Synchrotron radiation-based complementarytechniques [X-ray photorlectron spectroscopy and near-edge X-ray absorptionfinestructure (NEXAFS)] were used to characterize the electronic and molecularstructures of the complexes and the local structure around the copper ion (XAFS) inselected complexes. All complexes showed significant antitumor activity, proving tobe more effective than the reference drug cisplatin in a panel of human tumor celllines, and were able to overcome oxaliplatin and multidrug resistance. Noticeably,these Cu complexes appeared much more effective than cisplatin against 3Dspheroids of pancreatic PSN-1 cancer cells; among these, PPh3-containing Cu(I)complex15appeared to be the most promising derivative. Mechanistic studies revealed that15induced cancer cell death by means of an apoptosis-alternative cell death

Název v anglickém jazyce

Cu(I) and Cu(II) Complexes Based on Lonidamine-Conjugated Ligands Designed to Promote Synergistic Antitumor Effects

Popis výsledku anglicky

Bis(pyrazol-1-yl)- and bis(3,5-dimethylpyrazol-1-yl)-acetates were conjugated with the 2-hydroxyethylester and 2-aminoethylamide derivatives of the antineoplastic drug lonidamine to prepare Cu(I) and Cu(II) complexes that mightact through synergistic mechanisms of action due to the presence of lonidamine and copper in the same chemical entity. Synchrotron radiation-based complementarytechniques [X-ray photorlectron spectroscopy and near-edge X-ray absorptionfinestructure (NEXAFS)] were used to characterize the electronic and molecularstructures of the complexes and the local structure around the copper ion (XAFS) inselected complexes. All complexes showed significant antitumor activity, proving tobe more effective than the reference drug cisplatin in a panel of human tumor celllines, and were able to overcome oxaliplatin and multidrug resistance. Noticeably,these Cu complexes appeared much more effective than cisplatin against 3Dspheroids of pancreatic PSN-1 cancer cells; among these, PPh3-containing Cu(I)complex15appeared to be the most promising derivative. Mechanistic studies revealed that15induced cancer cell death by means of an apoptosis-alternative cell death

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

10305 - Fluids and plasma physics (including surface physics)

Projekt

—

Návaznosti

—

Rok uplatnění

2022

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Inorganic Chemistry

ISSN

0020-1669

e-ISSN

1520-510X

Svazek periodika

61

Číslo periodika v rámci svazku

12

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

19

Strana od-do

4919-4937

Kód UT WoS článku

000779822100013

EID výsledku v databázi Scopus

2-s2.0-85127248616