Academic Journal
New oxa/thiadiazole-chalcone hybrids linked via a clickable 1,2,3-triazole bridge with dual EGFR/VEGFR-2 kinase inhibitory activity and antiproliferative effects.
| Τίτλος: | New oxa/thiadiazole-chalcone hybrids linked via a clickable 1,2,3-triazole bridge with dual EGFR/VEGFR-2 kinase inhibitory activity and antiproliferative effects. |
|---|---|
| Συγγραφείς: | El-Qommos M; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Badr University in Assiut (BUA), Assiut 71511, Egypt. Electronic address: merit.nashaat@bua.edu.eg., Morsy RMI; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt. Electronic address: rana.morsy@aun.edu.eg., Abdel-Rahman HM; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Badr University in Assiut (BUA), Assiut 71511, Egypt; Department of Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt. Electronic address: hamdy.abdelrahman@bua.edu.eg., Hussein MA; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt. Electronic address: mhussein63@aun.edu.eg., Mostafa YA; Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt; Pharmaceutical Chemistry Department, Faculty of Pharmacy, Badr University in Assiut (BUA), Assiut 71511, Egypt. Electronic address: yaabdelkarem@pharm.aun.edu.eg. |
| Πηγή: | Bioorganic chemistry [Bioorg Chem] 2026 Oct 15; Vol. 182, pp. 110453. Date of Electronic Publication: 2026 Aug 31. |
| Τύπος έκδοσης: | Journal Article |
| Γλώσσα: | English |
| Στοιχεία περιοδικού: | Publisher: Elsevier Country of Publication: United States NLM ID: 1303703 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1090-2120 (Electronic) Linking ISSN: 00452068 NLM ISO Abbreviation: Bioorg Chem Subsets: MEDLINE |
| Imprint Name(s): | Publication: Amsterdam : Elsevier Original Publication: New York, London, Academic Press. |
| Ιατρικοί όροι (MeSH): | Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry , Antineoplastic Agents*/chemical synthesis , Vascular Endothelial Growth Factor Receptor-2*/antagonists & inhibitors , Vascular Endothelial Growth Factor Receptor-2*/metabolism , Triazoles*/chemistry , Triazoles*/pharmacology , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemistry , Protein Kinase Inhibitors*/chemical synthesis , Chalcone*/chemistry , Chalcone*/pharmacology , Thiadiazoles*/chemistry , Thiadiazoles*/pharmacology , Chalcones*/chemistry , Chalcones*/pharmacology, ErbB Receptors/antagonists & inhibitors ; ErbB Receptors/metabolism ; Cell Proliferation/drug effects ; Humans ; Structure-Activity Relationship ; Drug Screening Assays, Antitumor ; Molecular Structure ; Dose-Response Relationship, Drug ; Cell Line, Tumor ; Click Chemistry |
| Περίληψη: | The growing global incidence of cancer, coupled with the limitations of many current therapies, such as cytotoxicity, resistance, and poor selectivity, drives the need for new therapeutic agents. In this study, a novel series of pyridine-1,3,4-oxa/thiadiazole-chalcone hybrids, linked via a clickable 1,2,3-triazole moiety (7a-k and 8a-d), were synthesized and elucidated by FT-IR, NMR, and HRMS. These target compounds were screened in vitro for anticancer activity against three human cancer cell lines (A549, MCF-7, HCT-116) and for EGFR/VEGFR-2 inhibitory activity. The HCT-116 cells were the most sensitive. Notably, compounds 7b,7d, 7j, 8b, and 8d exhibited promising cytotoxic activity with IC (Copyright © 2026 Elsevier Inc. All rights reserved.) |
| Competing Interests: | 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. |
| Contributed Indexing: | Keywords: Anticancer; Click chemistry; Computational studies; Dual inhibition; Hybrids; Thiadiazole |
| Substance Nomenclature: | EC 2.7.10.1 (ErbB Receptors) 0 (Antineoplastic Agents) EC 2.7.10.1 (Vascular Endothelial Growth Factor Receptor-2) 0 (Triazoles) 0 (Protein Kinase Inhibitors) EC 2.7.10.1 (EGFR protein, human) EC 2.7.10.1 (KDR protein, human) 5S5A2Q39HX (Chalcone) 0 (Thiadiazoles) 0 (Chalcones) |
| Entry Date(s): | Date Created: 20260909 Date Completed: 20261008 Latest Revision: 20261008 |
| Update Code: | 20261008 |
| DOI: | 10.1016/j.bioorg.2026.110453 |
| PMID: | 42715623 |
| Βάση Δεδομένων: | MEDLINE |
| ISSN: | 1090-2120 |
|---|---|
| DOI: | 10.1016/j.bioorg.2026.110453 |