J 2023

Ternary copper(ii) complexes of 1,10-phenanthroline and coumarin-based oxylacetates as pro-apoptotic UPR CHOP inducers

MASURI, Sebastiano, Maria Grazia CABIDDU, Lukáš MORÁŇ, Tereza VESSELÁ, Martin BARTOSIK et. al.

Basic information

Original name

Ternary copper(ii) complexes of 1,10-phenanthroline and coumarin-based oxylacetates as pro-apoptotic UPR CHOP inducers

Authors

MASURI, Sebastiano, Maria Grazia CABIDDU, Lukáš MORÁŇ (203 Czech Republic, belonging to the institution), Tereza VESSELÁ (203 Czech Republic, belonging to the institution), Martin BARTOSIK, Josef HAVEL (203 Czech Republic, belonging to the institution), Francesca MELONI, Enzo CADONI, Petr VAŇHARA (203 Czech Republic, belonging to the institution) and Tiziana PIVETTA

Edition

New Journal of Chemistry, Cambridge, ROYAL SOC. CHEMISTRY, 2023, 1144-0546

Other information

Language

English

Type of outcome

Článek v odborném periodiku

Field of Study

10400 1.4 Chemical sciences

Country of publisher

United Kingdom of Great Britain and Northern Ireland

Confidentiality degree

není předmětem státního či obchodního tajemství

References:

Impact factor

Impact factor: 3.300 in 2022

RIV identification code

RIV/00216224:14110/23:00132615

Organization unit

Faculty of Medicine

UT WoS

001037416900001

Keywords in English

BIOLOGICAL-ACTIVITY; CYTOTOXIC ACTIVITY; CRYSTAL-STRUCTURE; SDNA-BINDING; CELL-DEATH; CISPLATINPLATINUM; LIGANDS; SYSTEM; ACID

Tags

Tags

International impact, Reviewed
Změněno: 22/7/2024 09:56, Mgr. Pavla Foltynová, Ph.D.

Abstract

V originále

We prepared six complexes with the formula [Cu(phen)(2)(Lx)](ClO4)(x: 1-6), where auxiliary ligands Lx are coumarin carboxylate derivatives bearing an oxylacetate moiety in the 6th or 7th position and different substituents in the 3rd or 4th position. Complexes show a pentacoordinated geometry around a metal ion. The possibility to complete the coordination sphere in an octahedral geometry makes the molecule able to further react. Complexes show affinity toward DNA mainly through electrostatic interactions and groove binding, while the interactions with DNA base pairs are guaranteed by the auxiliary ligands. The heteroleptic Cu(ii) complexes show cytotoxic activity in the micromolar concentration range, and mechanistic studies have shown how they can interfere at the endothelial reticulum level inducing the pro-apoptotic branch of the unfolded protein response (UPR). The actin-normalized CHOP to BiP density ratios suggest that the novel compounds induce preferentially the pro-apoptotic UPR signalling driven by the CHOP, in a dose-dependent way and according to the substituents in the coumarin moiety.

Links

ROZV/28/LF/2020, interní kód MU
Name: LF - Příspěvek na InstP 2020
Investor: Ministry of Education, Youth and Sports of the CR, Internal development projects