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, Pages 1121-1136 PDF (879.56 K) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ejchem.2022.150145.6506 | ||
| Authors | ||
| Eman G. Said1; Mohammed T. Elsaadi1, 2; Asmaa A. Mohammed* 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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