Synthesis, Docking and Biological Evaluation of 2,4- Disubstituted Quinazolines With Multi-Target Activities as Anti-cancer and Antimicrobial Agents
El-Saadi, M., Amin, N., zaki, S., abdelrahman, H. (2020). Synthesis, Docking and Biological Evaluation of 2,4- Disubstituted Quinazolines With Multi-Target Activities as Anti-cancer and Antimicrobial Agents. EKB Journal Management System, 63(10), 3721-3734. doi: 10.21608/ejchem.2020.23300.2385
Mohammed T El-Saadi; Noha H Amin; shimaa saeed zaki; hamdy mohamed abdelrahman. "Synthesis, Docking and Biological Evaluation of 2,4- Disubstituted Quinazolines With Multi-Target Activities as Anti-cancer and Antimicrobial Agents". EKB Journal Management System, 63, 10, 2020, 3721-3734. doi: 10.21608/ejchem.2020.23300.2385
El-Saadi, M., Amin, N., zaki, S., abdelrahman, H. (2020). 'Synthesis, Docking and Biological Evaluation of 2,4- Disubstituted Quinazolines With Multi-Target Activities as Anti-cancer and Antimicrobial Agents', EKB Journal Management System, 63(10), pp. 3721-3734. doi: 10.21608/ejchem.2020.23300.2385
El-Saadi, M., Amin, N., zaki, S., abdelrahman, H. Synthesis, Docking and Biological Evaluation of 2,4- Disubstituted Quinazolines With Multi-Target Activities as Anti-cancer and Antimicrobial Agents. EKB Journal Management System, 2020; 63(10): 3721-3734. doi: 10.21608/ejchem.2020.23300.2385

Synthesis, Docking and Biological Evaluation of 2,4- Disubstituted Quinazolines With Multi-Target Activities as Anti-cancer and Antimicrobial Agents

Egyptian Journal of Chemistry
Article 12, Volume 63, Issue 10, October 2020, Page 3721-3734  XML PDF (1017.46 K)
Document Type: Original Article
DOI: 10.21608/ejchem.2020.23300.2385
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Authors
Mohammed T El-Saadi1; Noha H Amin2; shimaa saeed zaki email 3; hamdy mohamed abdelrahman4
1Department of Medicinal Chemistry, Faculty of Pharmacy, Sinai University, Qantara, Egypt
2Department of Medicinal Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62111, Egypt
3Medicinal chemistry department, faculty of pharmacy, beni suef university, benisuef, egypt
4Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Nahda University, Beni-suef, Egypt
Abstract
A series of 2,4-disubstituted quinazoline derivatives was designed and synthesized as multi-target therapeutic agents that may act as anti-cancer and antimicrobial agents. The target compounds were evaluated for primary anti-cancer activity followed by EGFR inhibition assay for most potent compounds. Compounds 6 and 8c exhibited good EGFR inhibition activity with IC50 values of 0.201 and 0.405 µM, respectively, in comparison to lapatinib as a reference with IC50 value of 0.115 µM. Docking study of the synthesized compounds into the binding site of EGFR tyrosine kinase was performed to compare the binding mode of these compounds to the known EGFR inhibitor, lapatinib. Moreover, antimicrobial activity, cytotoxity and hemolytic analysis were estimated according to CO-ADD (The Community for Antimicrobial Drug Discovery) procedures. Compounds 4 and 5c possessed potent antifungal activity with minimum inhibitory concentration (MIC) values of 8 and 4 µg/mL against C. albicans and C. neoformance, respectively, compared to fluconazole as a reference drug with MIC values of 0.125 and 8 µg/mL against same fungi.
Keywords
Quinazoline; antitumor activity; EGFR assay; antimicrobial activity
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