Synthesis of novel nicotinic acid derivatives of potential antioxidant and anticancer activity.


Journal

Archiv der Pharmazie
ISSN: 1521-4184
Titre abrégé: Arch Pharm (Weinheim)
Pays: Germany
ID NLM: 0330167

Informations de publication

Date de publication:
Dec 2023
Historique:
revised: 10 09 2023
received: 08 05 2023
accepted: 13 09 2023
medline: 4 12 2023
pubmed: 4 10 2023
entrez: 4 10 2023
Statut: ppublish

Résumé

This study comprises the design and synthesis of novel nicotinic acid-based cytotoxic agents with selective inhibitory efficacy against the vascular endothelial growth factor receptor-2 (VEGFR-2). Screening of novel compounds for cytotoxicity was assessed against 60 human cancer cell lines. The two most active compounds, 5b and 5c, and the reference drugs sorafenib and doxorubicin were investigated against HCT-15, PC-3, and CF-295 cancer cell lines. Compound 5c exhibited the highest cytotoxic potential compared to doxorubicin against the HCT-15 and PC-3 tumor cell lines. Moreover, it exhibited higher cytotoxic potential and selectivity toward the HCT-15 cell panel compared with sorafenib. Compound 5c demonstrated promising VEGFR-2 inhibition (concentration needed to inhibit cell viability by 50%, IC

Identifiants

pubmed: 37792247
doi: 10.1002/ardp.202300250
doi:

Substances chimiques

Sorafenib 9ZOQ3TZI87
Vascular Endothelial Growth Factor Receptor-2 EC 2.7.10.1
Niacin 2679MF687A
Antioxidants 0
Vascular Endothelial Growth Factor A 0
Protein Kinase Inhibitors 0
Antineoplastic Agents 0
Doxorubicin 80168379AG
Superoxide Dismutase EC 1.15.1.1

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

e2300250

Subventions

Organisme : None

Informations de copyright

© 2023 Deutsche Pharmazeutische Gesellschaft.

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Auteurs

Yara El-Dash (Y)

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

Nadia A Khalil (NA)

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

Eman M Ahmed (EM)

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

Soha O Hassanin (SO)

Biochemistry Department, Faculty of Pharmacy, Modern University for Technology and Information (MTI), Cairo, Egypt.

Ayah M H Gowifel (AMH)

Pharmacology and Toxicology Department, Faculty of Pharmacy, Modern University for Technology and Information (MTI), Cairo, Egypt.

Marwa S A Hassan (MSA)

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

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