New substituted benzoxazine derivatives as potent inducers of membrane permeability and cell death.

Antitumor Benzoxazines Cell death Membrane permeability and cell cycle arrest

Journal

Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298

Informations de publication

Date de publication:
24 Jul 2024
Historique:
received: 20 06 2024
revised: 17 07 2024
accepted: 22 07 2024
medline: 29 7 2024
pubmed: 29 7 2024
entrez: 28 7 2024
Statut: aheadofprint

Résumé

The search for new agents targeting different forms of cell death is an important research focus for developing new and potent antitumor therapies. As a contribution to this endeavor, we have designed and synthesized a series of new substituted 3,4-dihydro-2H-1,4-benzoxazine derivatives. These compounds have been evaluated for their efficacy against MCF-7 breast cancer and HCT-116 colon cancer cell lines. Overall, substituting this heterocycle led to improved antiproliferative activity compared to the unsubstituted derivative 1. The most active compounds, 2b and 4b, showed IC

Identifiants

DOI: 10.1016/j.bmc.2024.117849 PMID: 39068873
pubmed: 39068873
pii: S0968-0896(24)00263-3
doi: 10.1016/j.bmc.2024.117849
pii:
doi:

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

117849

Informations de copyright

Copyright © 2024 The Authors. Published by Elsevier Ltd.. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Auteurs

Ana Conejo-García (A)

Department of Medicinal and Organic Chemistry and Excellence Research Unit of Chemistry Applied to Biomedicine and the Environment, Faculty of Pharmacy, Campus Cartuja s/n, University of Granada, 18071 Granada, Spain; Biosanitary Institute of Granada (ibs.GRANADA), SAS-University of Granada, Avenida de Madrid, 15, 18012 Granada, Spain.

Yaiza Jiménez-Martínez (Y)

Department of Anatomy and Human Embryology, Faculty of Medicine, Avenida de la Investigación 11, University of Granada, 18016 Granada, Spain; Biopathology and Regenerative Medicine Institute (IBIMER), Avenida del Conocimiento s/n, 18016 Granada, Spain.

Rubén Cámara (R)

Department of Medicinal and Organic Chemistry and Excellence Research Unit of Chemistry Applied to Biomedicine and the Environment, Faculty of Pharmacy, Campus Cartuja s/n, University of Granada, 18071 Granada, Spain.

Francisco Franco-Montalbán (F)

Department of Medicinal and Organic Chemistry and Excellence Research Unit of Chemistry Applied to Biomedicine and the Environment, Faculty of Pharmacy, Campus Cartuja s/n, University of Granada, 18071 Granada, Spain.

Jesús Peña-Martín (J)

Department of Anatomy and Human Embryology, Faculty of Medicine, Avenida de la Investigación 11, University of Granada, 18016 Granada, Spain; Biopathology and Regenerative Medicine Institute (IBIMER), Avenida del Conocimiento s/n, 18016 Granada, Spain.

Houria Boulaiz (H)

Biosanitary Institute of Granada (ibs.GRANADA), SAS-University of Granada, Avenida de Madrid, 15, 18012 Granada, Spain; Department of Anatomy and Human Embryology, Faculty of Medicine, Avenida de la Investigación 11, University of Granada, 18016 Granada, Spain; Biopathology and Regenerative Medicine Institute (IBIMER), Avenida del Conocimiento s/n, 18016 Granada, Spain. Electronic address: hboulaiz@ugr.es.

M Dora Carrión (MD)

Department of Medicinal and Organic Chemistry and Excellence Research Unit of Chemistry Applied to Biomedicine and the Environment, Faculty of Pharmacy, Campus Cartuja s/n, University of Granada, 18071 Granada, Spain; Biosanitary Institute of Granada (ibs.GRANADA), SAS-University of Granada, Avenida de Madrid, 15, 18012 Granada, Spain. Electronic address: dcarrion@ugr.es.

Classifications MeSH