New Metal-Based Drugs for Cancer Treatment: Single Molecules, Nanomaterials, and Beyond

Topic Information

Dear Colleagues,

The search for new therapeutic alternatives to combat cancer has found in the transition elements a very abundant source of compounds and nanostructures with different geometric arrangements and reactivity that provide unique opportunities to interact with varying sites of recognition and exert mechanisms of action other than those drugs that are currently used to kill tumor cells. These features not only provide new tools independently but also could provide advantages enhancing concomitantly or sequentially the effect of known antineoplastic agents. In this Topic, the most recent findings regarding preclinical studies of metallodrugs, including but not limited to synthesis, characterization, simulation, computational modeling, and theoretical approach to new antiproliferative and antitumor agents, qualitative/quantitative structure-activity studies, bio-speciation/bioaccumulation, interaction with specific enzymes and nucleic acids, cytotoxicity, genotoxicity, teratogenicity, and general toxicity will be outlined. Submissions of original papers and focused reviews are welcome.

Dr. Juan Carlos García-Ramos
Dr. Yanis Toledano-Magaña
Dr. Gener José Avilés Rodríguez
Dr. Rodrigo Galindo-Murillo
Topic Editors

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Participating Journals

Journal Name	Impact Factor	CiteScore	Launched Year	First Decision (median)	APC
Biomedicines biomedicines	4.7	3.7	2013	15.4 Days	CHF 2600
Cancers cancers	5.2	7.4	2009	17.9 Days	CHF 2900
Future Pharmacology futurepharmacol	-	-	2021	20.5 Days	CHF 1000
Journal of Clinical Medicine jcm	3.9	5.4	2012	17.9 Days	CHF 2600
Pharmaceutics pharmaceutics	5.4	6.9	2009	14.2 Days	CHF 2900

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All Biomedicines Cancers Future Pharmacology JCM Pharmaceutics

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Open AccessArticle

Heteroleptic Copper(II) Complexes Containing 2′-Hydroxy-4-(Dimethylamino)Chalcone Show Strong Antiproliferative Activity

by Zdeněk Trávníček, Tomáš Malina, Ján Vančo, Marek Šebela and Zdeněk Dvořák

Pharmaceutics 2023, 15(2), 307; https://doi.org/10.3390/pharmaceutics15020307 - 17 Jan 2023

Cited by 2 | Viewed by 1604

Abstract

A series of six heteroleptic copper(II) complexes with 2′-hydroxy-4-(dimethylamino)chalcone (HL) with the composition [Cu(N-N)(L)]NO₃ (1–6), where N-N stands for dmbpy = 5,5′-dimethyl-2,2′-bipyridine (1), bphen = 4,7-diphenyl-1,10-phenanthroline (2), dbbpy = 4,4′-di-tert-butyl-2,2′-bipyridine (3 [...] Read more.

A series of six heteroleptic copper(II) complexes with 2′-hydroxy-4-(dimethylamino)chalcone (HL) with the composition [Cu(N-N)(L)]NO₃ (1–6), where N-N stands for dmbpy = 5,5′-dimethyl-2,2′-bipyridine (1), bphen = 4,7-diphenyl-1,10-phenanthroline (2), dbbpy = 4,4′-di-tert-butyl-2,2′-bipyridine (3), nphen = 5-nitro-1,10-phenanthroline (4), bpy = 2,2′-bipyridine, (5), and dpa = 2,2′-dipyridylamine (6), was prepared and thoroughly characterized. The in vitro cytotoxicity screening on eight human cancer cell lines identified complex 2, containing the bulkiest N-donor ligands (bphen) as highly cytotoxic against cancer cells, with IC₅₀ values ranking from 1.0 to 2.3 μM, with good selectivity and low toxicity against healthy human fetal lung fibroblasts MRC-5. The cell-based assays, involving the most effective complex 2 in A2780 cancer cells, revealed its strong pro-apoptotic effects based on the effective activation of caspases 3/7, ROS overproduction, and autophagy in the A2780 cells while not impeding the cell cycle and mitochondrial membrane functions. The cellular uptake studies in A2780 and 22Rv1 cells uncovered no intracellular transport of the cationic complex 2, supporting the hypothesis that the in vitro anticancer effects of complex 2 are based on the combined extrinsic activation of apoptosis and autophagy induction. Full article

(This article belongs to the Topic New Metal-Based Drugs for Cancer Treatment: Single Molecules, Nanomaterials, and Beyond)

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