Year: 2024
Type: article
Abstract: High Resolution Image Download MS PowerPoint Slide Cu(II) complexes with 2,2′:6′,2″-terpyridines (terpy) and 2,6-bis(thiazol-2-yl)pyridines (dtpy) with 1- or 2-naphtyl and methoxy-naphtyl were synthesized to elucidate the impact of the triimine core, naphtyl linking mode, and presence of methoxy groups on the antiproliferative activity of [CuCl 2 (L n )]. Their antiproliferative effect was analyzed in ovarian (A2780) and colorectal (HCT116) carcinomas and colorectal carcinoma resistant to doxorubicin (HCT116-DoxR) cell lines and in normal human fibroblasts. Among all complexes, the 1- and 2-naphtyl substituted terpy Cu(II) complexes ( Cu1a and Cu1b ) showed the strongest cytotoxicity, namely, in HCT116-DoxR 2Dcells and were also capable of inducing the loss of cell viability in 3D HCT116-DoxR spheroids. Their intracellular localization, capability to increase reactive oxygen species (ROS), and interaction with DNA (nonintercalative mode) trigger oxidative DNA cleavage leading to cell death by apoptosis and autophagy. Cu1a and Cu1b do not show in vivo toxicity in a chicken embryo and can interact with bovine serum albumin (BSA).
Source: Journal of Medicinal Chemistry
Language: English
Subfield: Oncology
Field: Medicine
Domain: Health Sciences
Open Access status: hybrid
Estimated APC paid: $4,500
Awards: Unidade de Ciências Biomoleculares Aplicadas, G3926179308, Unidade de Ciências Biomoleculares Aplicadas, Instituto para a Saúde e a Bioeconomia, (Gold4TME): Modulation of tumor microenvironment via combinatorial gold nanomedicines, NANOHEAT – Nanopartículas de ouro para potenciar a ablação fototérmica em cacnro colorectal
OpenAlex ID: W4404025268