Design, Synthesis and Molecular Docking Studies of Novel Amino Acids and Peptide Derivatives Based on Phthaloyl Chloride With Expected Anticancer Activity.
Mohamed, F., O. Moustafa, G., Nossier, E., Mounier, M. (2024). Design, Synthesis and Molecular Docking Studies of Novel Amino Acids and Peptide Derivatives Based on Phthaloyl Chloride With Expected Anticancer Activity.. EKB Journal Management System, 67(13), 577-587. doi: 10.21608/ejchem.2024.258560.9093
Fatma Hassan Mohamed; Gaber O. Moustafa; Eman Nossier; Marwa Mounier. "Design, Synthesis and Molecular Docking Studies of Novel Amino Acids and Peptide Derivatives Based on Phthaloyl Chloride With Expected Anticancer Activity.". EKB Journal Management System, 67, 13, 2024, 577-587. doi: 10.21608/ejchem.2024.258560.9093
Mohamed, F., O. Moustafa, G., Nossier, E., Mounier, M. (2024). 'Design, Synthesis and Molecular Docking Studies of Novel Amino Acids and Peptide Derivatives Based on Phthaloyl Chloride With Expected Anticancer Activity.', EKB Journal Management System, 67(13), pp. 577-587. doi: 10.21608/ejchem.2024.258560.9093
Mohamed, F., O. Moustafa, G., Nossier, E., Mounier, M. Design, Synthesis and Molecular Docking Studies of Novel Amino Acids and Peptide Derivatives Based on Phthaloyl Chloride With Expected Anticancer Activity.. EKB Journal Management System, 2024; 67(13): 577-587. doi: 10.21608/ejchem.2024.258560.9093

Design, Synthesis and Molecular Docking Studies of Novel Amino Acids and Peptide Derivatives Based on Phthaloyl Chloride With Expected Anticancer Activity.

Egyptian Journal of Chemistry
Volume 67, Issue 13, December 2024, Page 577-587  XML PDF (709.14 K)
Document Type: Original Article
DOI: 10.21608/ejchem.2024.258560.9093
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Authors
Fatma Hassan Mohamed1; Gaber O. Moustafa email 2; Eman Nossier3; Marwa Mounier4
1Peptide Chemistry Department, National Research Centre, Dokki 12622, Cairo, Egypt
2Peptide Chemistry Department, Chemical Industries Research Division, National Research Centre, 12622-Dokki, Cairo, Egypt.
3Pharmaceutical Chemistry Department, Faculty of Pharmacy, Al-Azhar University (Girls), Cairo 12622, Egypt
4Pharmaceutical and Drug Industries Research Division, Department of Pharmacognosy, National Research Centre, Giza, Egypt
Abstract
This paper discusses the synthesis and characterization of Nα-phthaloyl)-bis-[amino acid]-X, Nα-phthaloyl)-bis-[dipeptide]-X derivatives were conducted, followed by a cytotoxicity evaluation against human cancer cell lines. Compounds 12 and 16 exhibited notable cytotoxic activity against the human colon (CaCo-2) cancer cell line. Molecular docking of these promising derivatives (12 and 16) revealed favorable binding within the active site of the EGFR enzyme, suggesting potential anticancer activity. These docking results suggest a well-fitted interaction involving diverse hydrogen bond interactions with protein residues, indicating a potential for eliciting anticancer activity through this mechanism. This comprehensive approach integrates synthesis, cytotoxicity evaluation, and molecular docking, providing valuable insights into the anticancer properties of these compounds, especially against colon cancer cells.
Keywords
amino acid; linear peptide; cyclic pentapeptide; Nα -phthaloyl-bis-peptides; cytotoxicity
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