Synthesis, Biological Evaluation and Molecular Docking Studies of Newly Synthesized 4- Amino Quinazoline Derivatives as Potential Multitarget Anticancer Agents.
Said, E., Elsaadi, M., Mohammed, A., Amin, N. (2022). Synthesis, Biological Evaluation and Molecular Docking Studies of Newly Synthesized 4- Amino Quinazoline Derivatives as Potential Multitarget Anticancer Agents.. EKB Journal Management System, 65(131), 1121-1136. doi: 10.21608/ejchem.2022.150145.6506
Eman G. Said; Mohammed T. Elsaadi; Asmaa A. Mohammed; Noha H. Amin. "Synthesis, Biological Evaluation and Molecular Docking Studies of Newly Synthesized 4- Amino Quinazoline Derivatives as Potential Multitarget Anticancer Agents.". EKB Journal Management System, 65, 131, 2022, 1121-1136. doi: 10.21608/ejchem.2022.150145.6506
Said, E., Elsaadi, M., Mohammed, A., Amin, N. (2022). 'Synthesis, Biological Evaluation and Molecular Docking Studies of Newly Synthesized 4- Amino Quinazoline Derivatives as Potential Multitarget Anticancer Agents.', EKB Journal Management System, 65(131), pp. 1121-1136. doi: 10.21608/ejchem.2022.150145.6506
Said, E., Elsaadi, M., Mohammed, A., Amin, N. Synthesis, Biological Evaluation and Molecular Docking Studies of Newly Synthesized 4- Amino Quinazoline Derivatives as Potential Multitarget Anticancer Agents.. EKB Journal Management System, 2022; 65(131): 1121-1136. doi: 10.21608/ejchem.2022.150145.6506

Synthesis, Biological Evaluation and Molecular Docking Studies of Newly Synthesized 4- Amino Quinazoline Derivatives as Potential Multitarget Anticancer Agents.

Egyptian Journal of Chemistry
Volume 65, Issue 131, December 2022, Page 1121-1136  XML PDF (879.56 K)
Document Type: Original Article
DOI: 10.21608/ejchem.2022.150145.6506
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Authors
Eman G. Said1; Mohammed T. Elsaadi1, 2; Asmaa A. Mohammed email 1; Noha H. Amin1
1Department of Medicinal Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62514, Egypt
2Department of Medicinal Chemistry, Faculty of Pharmacy, Sinai University, Kantra, Egypt.
Abstract
A series of 4-aminoquinazoline linked to cyanopyrimidine derivatives (6a-c and 7a-f) was designed, synthesized with good yields and screened at National Cancer Institute (NCI)-disease oriented anticancer screen protocol against nine panel of cancer cell lines. Comprehensively, the structures of the synthesized compounds were confirmed by different spectroscopic methods like melting points, H1- NMR, 13C- NMR and HRMS, Moreover, the most active compound 7a was selected for in vitro enzyme inhibitory activities against epidermal growth factor receptor and cyclin dependent kinase-2 enzymes. Cell cycle analysis and apoptosis were evaluated on three different cancerous cells; UO-31, MCF-7 and IGROV-1. Finally, the molecular modelling for compound 7a inside the ATP binding site of epidermal growth factor receptor and cyclin dependent kinase-2 enzymes was performed to predict the binding mode to the active site of these enzymes using lapatinib and ribociclib as standards respectively. Our research found that quinazoline-containing cyano pyrimidine derivatives were promising cytotoxic agents for further study.
Keywords
Amino quinazolines; Multi target antitumor; Molecular Docking; apoptosis
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