Cited by Fragment-based design and synthesis of coumarin-based thiazoles as dual c-MET/STAT-3 inhibitors for potential antitumor agents

The current landscape of 1,2,3‐triazole hybrids with anticancer therapeutic potential: Part I DOI

Shanshan Huang,

Zhi Xu,

Yafei Zhuang

et al.

Archiv der Pharmazie, Journal Year: 2025, Volume and Issue: 358(3)

Published: March 1, 2025

Abstract Cancer, with its steadily increasing morbidity and mortality, will continue to pose a threat humanity over an extended period. Chemotherapeutics play indispensable role in cancer treatment, hundreds of drugs have been approved for this purpose. Nevertheless, the fight against remains formidable challenge. This is mainly due emergence multidrug resistance severe side effects associated currently available anticancer drugs. Consequently, there urgent imperative explore novel chemotherapeutic agents. 1,2,3‐Triazoles belong one most privileged classes nitrogen‐containing five‐membered heterocycles are regarded as prominent sources development innovative chemotherapeutics. 1,2,3‐Triazole hybrids, which possess multitargeted mechanisms action within progression pathway, hold potential overcome mitigate effects. Furthermore, several 1,2,3‐triazole hybrids already therapy or under clinical evaluation. clearly demonstrates that valuable scaffolds treatment eradication cancer. review aims provide insights into therapeutic along their action, crucial aspects design, structure–activity relationships (SARs). It encompasses articles published from 2021 onward.

Language: Английский

Citations

Discovery of 1-phenyl-1,2,3-triazole ureas as dual VEGFR-2/JNK-1 type II kinase inhibitors targeting pancreatic cancer DOI

Wagdy M. Eldehna, Eslam Roshdy,

Maha-Hamadien Abdulla

et al.

International Journal of Biological Macromolecules, Journal Year: 2025, Volume and Issue: unknown, P. 142372 - 142372

Published: March 1, 2025

Language: Английский

Citations

Shooting an Arrow against Convulsion: Novel Triazole-Grafted Benzenesulfonamide Derivatives as Carbonic Anhydrase II and VII Inhibitors DOI

Mohamed A. Zeidan,

Mahmoud Abdelrahman Alkabbani, Simone Giovannuzzi

et al.

Journal of Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown

Published: April 16, 2025

This study investigates new anticonvulsant substances that target the epilepsy-associated carbonic anhydrase isoforms II and VII. The 1,2,3-triazole with a benzenesulfonamide motif is present in produced molecules. Of these, 5b 5c exhibited remarkable selectivity inhibitory efficacy toward hCA VII over I. KI values of were 6.3 10.1 nM, respectively, 21.6 18.9 respectively. In pilocarpine-induced paradigm, vivo assessments showed decreased seizure severity susceptibility delayed onset diminished intensity. quick absorption stability demonstrated by pharmacokinetic investigations. Evaluations toxicity no neurotoxic effects high safety margin (LD50 > 2000 mg/kg). Mechanistic research has shown effectiveness maintaining neuronal integrity, reducing mTOR activation, raising hippocampus KCC2 levels. Compound 5b's binding interactions clarified docking dynamics experiments.

Language: Английский

Citations

Novel benzofuran-conjugated indolin-2-ones as anticancer agents; design, synthesis, biological assessments, and molecular modeling insights DOI

Wagdy M. Eldehna, Haytham O. Tawfik, Mohamed S. Nafie

et al.

Bioorganic Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 108494 - 108494

Published: April 1, 2025

Language: Английский

Citations

Discovery of new quinoline derivatives bearing 1-aryl-1,2,3-triazole motif as influenza H1N1 virus neuraminidase inhibitors DOI

Ahmed Sabt, Eman F. Khaleel, Moataz A. Shaldam

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 151, P. 107703 - 107703

Published: Aug. 6, 2024

Language: Английский

Citations

Exploring antitumor activity of novel imidazo[2,1-b]thiazole and imidazo[1,2-a]pyridine derivatives on MDA-231 cell line: targeting VEGFR-2 enzyme with computational insight DOI

Mohamed K. Elgohary, Mahmoud S. Elkotamy, Sara T. Al‐Rashood

et al.

Journal of Molecular Structure, Journal Year: 2024, Volume and Issue: 1322, P. 140579 - 140579

Published: Nov. 3, 2024

Language: Английский

Citations

Recent Developments Towards the Synthesis of Triazole Derivatives: A Review DOI

Issam Ameziane El Hassani,

Khouloud Rouzi,

Anouar Ameziane El Hassani

et al.

Organics, Journal Year: 2024, Volume and Issue: 5(4), P. 450 - 471

Published: Oct. 24, 2024

The triazole scaffold is a crucial component of heterocyclic chemistry, serving as basic building block in organic synthesis, materials science, and medicinal chemistry. Triazole five-membered ring composed three nitrogen atoms two carbon atoms, it exists isomeric forms: 1,2,3-triazole 1,2,4-triazole. Compounds featuring the are important heterocycles known for their diverse biological activities, including antimicrobial, antiproliferative, antimalarial, anticonvulsant, anti-inflammatory, antineoplastic, antiviral, analgesic, anticancer properties. As result, derivatives have attracted significant attention from researchers. This review aims to provide thorough overview published studies on synthesis derivatives, highlighting various methods obtaining moiety. These include classical approaches well microwave ultrasound-assisted techniques.

Language: Английский

Citations

Spiro-fused indoline-quinazoline hybrids as smart bombs against TNF-α-mediated inflammation DOI

Mahmoud S. Elkotamy, Mohamed K. Elgohary, Mahmoud Abdelrahman Alkabbani

et al.

International Journal of Biological Macromolecules, Journal Year: 2024, Volume and Issue: 283, P. 137554 - 137554

Published: Nov. 15, 2024

Language: Английский

Citations

Fragment-based design and synthesis of coumarin-based thiazoles as dual c-MET/STAT-3 inhibitors for potential antitumor agents DOI

Bassem H. Naguib,

Heba A. Elsebaie,

Mohamed S. Nafie

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 151, P. 107682 - 107682

Published: Aug. 6, 2024

Language: Английский

Citations