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Dual EGFR and telomerase inhibitory potential of new triazole tethered Schiff bases endowed with apoptosis: design, synthesis, and biological assessments

Year: 2024
Type: article
Abstract: , respectively. Hence, protein expression of the apoptosis-related proteins was carried out for compound 5g. Pro-apoptotic proteins (caspases 3, 8, and 9) were upregulated by 1.35, 1.55, and 1.51-fold change, respectively. Meanwhile, the anti-apoptotic proteins (CDK-2, CDK-4, and CDK-6) were downregulated by 2.91, 2.01, and 9.15-fold change, respectively, ensuring the apoptotic potential of compound 5g. Accordingly, compound 5g was selected for further investigation of its effects on cell cycle progression in A375 cancer cells. Obviously, compound 5g prompted cell cycle arrest at the G0-G1 phase. Additionally, the investigated compounds showed eligible pharmacokinetic profiles with feasible oral bioavailability. Consequently, the synthesized compounds can be treated as lead multi-target anticancer ligands for future optimization.
DOI: 10.1039/d4md00750f
Authors: Mohamed A. Zeidan, Heba F. Ashour, Asmaa S. A. Yassen, Ayman Abo Elmaaty, Ayman B. Farag, Marwa Sharaky, Abdullah Yahya Abdullah Alzahrani, Mohammed H. AL Mughram, Ahmed A. Al-Karmalawy
Institutions: Horus University – Egypt, Galala University, Suez Canal University, Port Said University, Ahram Canadian University, Cairo University, King Khalid University, University of Mashreq
Language: English
Field: Chemistry
Open Access status: green
OpenAlex ID: W4405565486
FWCI: 2.867
Cites: 58
Cited by: 21
Related to: 10