Structure-activity relationship and cytotoxicity of the new thiosemicarbazide derivatives and their Cu(II) complexes against prostate and melanoma cancer cells.

Antimicrobial and anticancer activity Cu(II) complex FTIR spectroscopy Thiosemicarbazide derivative X-ray analysis

Journal

Archives of biochemistry and biophysics
ISSN: 1096-0384
Titre abrégé: Arch Biochem Biophys
Pays: United States
ID NLM: 0372430

Informations de publication

Date de publication:
07 Mar 2024
Historique:
received: 22 12 2023
revised: 15 02 2024
accepted: 06 03 2024
medline: 10 3 2024
pubmed: 10 3 2024
entrez: 9 3 2024
Statut: aheadofprint

Résumé

In this study, eighteen new ligands (B1-B18) containing a thiosemicarbazide core were synthesized and characterized in terms of physicochemical properties, molecular docking and in vitro biological activity. The structures of eleven ligands were investigated using X-Ray diffraction and Hirschfeld Surface analysis. To study the structure-activity relationship, the organic ligands contained pyridin-2-ylmethyl, pyridin-3-ylmethyl or pyridin-4-ylmethyl moieties and various substituents. Their pharmakokinetic profiles and molecular docking results suggest high potential as new drug candidates. The complexing ability of the selected organic ligands was also evaluated, yielding five new Cu(II) complexes (Cu(B1)Cl

Identifiants

DOI: 10.1016/j.abb.2024.109955 PMID: 38460659
pubmed: 38460659
pii: S0003-9861(24)00074-2
doi: 10.1016/j.abb.2024.109955
pii:
doi:

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

109955

Informations de copyright

Copyright © 2024. Published by Elsevier Inc.

Auteurs

Bartłomiej Rogalewicz (B)

Institute of General and Ecological Chemistry, Faculty of Chemistry, Lodz University of Technology, Żeromskiego 116, 90-924, Lodz, Poland. Electronic address: bartlomiej.rogalewicz@dokt.p.lodz.pl.

Monika Pitucha (M)

Independent Radiopharmacy Unit, Faculty of Pharmacy, Medical University of Lublin, Chodzki 4a, 20-093, Lublin, Poland.

Marcin Świątkowski (M)

Institute of General and Ecological Chemistry, Faculty of Chemistry, Lodz University of Technology, Żeromskiego 116, 90-924, Lodz, Poland.

Ewelina Humeniuk (E)

Independent Medical Biology Unit, Faculty of Pharmacy, Medical University of Lublin, Jaczewskiego 8b, 20-093, Lublin, Poland.

Grzegorz Adamczuk (G)

Independent Medical Biology Unit, Faculty of Pharmacy, Medical University of Lublin, Jaczewskiego 8b, 20-093, Lublin, Poland.

Monika Drózd (M)

Independent Radiopharmacy Unit, Faculty of Pharmacy, Medical University of Lublin, Chodzki 4a, 20-093, Lublin, Poland.

Zbigniew Karczmarzyk (Z)

Department of Chemistry, Siedlce University of Natural Sciences and Humanities, Ul. 3 Maja 54, 08-110, Siedlce, Poland.

Elżbieta Kuśmierek (E)

Institute of General and Ecological Chemistry, Faculty of Chemistry, Lodz University of Technology, Żeromskiego 116, 90-924, Lodz, Poland.

Krzysztof Strzelec (K)

Institute of Polymer & Dye Technology, Faculty of Chemistry, Lodz University of Technology, Stefanowskiego 12/16, 90-924, Lodz, Poland.

Anita Raducka (A)

Institute of General and Ecological Chemistry, Faculty of Chemistry, Lodz University of Technology, Żeromskiego 116, 90-924, Lodz, Poland.

Waldemar Wysocki (W)

Department of Chemistry, Siedlce University of Natural Sciences and Humanities, Ul. 3 Maja 54, 08-110, Siedlce, Poland.

Alina Olender (A)

Chair and Department of Medical Microbiology, Medical University of Lublin, Chodzki 1, 20-093, Lublin, Poland.

Anna Kozub (A)

Department of Bioanalytics, Faculty of Biomedicine, Medical University of Lublin, Jaczewskiego 8b, 20-090, Lublin, Poland.

Dorota Kowalczuk (D)

Chair and Department of Medicinal Chemistry, Faculty of Pharmacy, Medical University of Lublin, Jaczewskiego 4, 20-090, Lublin, Poland.

Ewa Poleszak (E)

Laboratory of Preclinical Testing, Chair and Department of Applied and Social Pharmacy, Medical University of Lublin, Chodzki 1, 20-093, Lublin, Poland.

Agnieszka Czylkowska (A)

Institute of General and Ecological Chemistry, Faculty of Chemistry, Lodz University of Technology, Żeromskiego 116, 90-924, Lodz, Poland. Electronic address: agnieszka.czylkowska@p.lodz.pl.

Classifications MeSH