Design, Synthesis and Molecular Docking Studies of Novel Cyclic Pentapeptides Based on Phthaloyl Chloride with Expected Anticancer Activity
Mohamed, F., Shalaby, A., Soliman, H., Abdelazem, A., Mounier, M., Nossier, E., Moustafa, G. (2020). Design, Synthesis and Molecular Docking Studies of Novel Cyclic Pentapeptides Based on Phthaloyl Chloride with Expected Anticancer Activity. EKB Journal Management System, 63(5), 1723-1736. doi: 10.21608/ejchem.2019.18452.2137
Fatma Hassan Mohamed; Ahmed Shalaby; Hanan abdelhameid Soliman; Ahmed Abdelazem; Marwa Mounier; Eman Nossier; Gaber Moustafa. "Design, Synthesis and Molecular Docking Studies of Novel Cyclic Pentapeptides Based on Phthaloyl Chloride with Expected Anticancer Activity". EKB Journal Management System, 63, 5, 2020, 1723-1736. doi: 10.21608/ejchem.2019.18452.2137
Mohamed, F., Shalaby, A., Soliman, H., Abdelazem, A., Mounier, M., Nossier, E., Moustafa, G. (2020). 'Design, Synthesis and Molecular Docking Studies of Novel Cyclic Pentapeptides Based on Phthaloyl Chloride with Expected Anticancer Activity', EKB Journal Management System, 63(5), pp. 1723-1736. doi: 10.21608/ejchem.2019.18452.2137
Mohamed, F., Shalaby, A., Soliman, H., Abdelazem, A., Mounier, M., Nossier, E., Moustafa, G. Design, Synthesis and Molecular Docking Studies of Novel Cyclic Pentapeptides Based on Phthaloyl Chloride with Expected Anticancer Activity. EKB Journal Management System, 2020; 63(5): 1723-1736. doi: 10.21608/ejchem.2019.18452.2137

Design, Synthesis and Molecular Docking Studies of Novel Cyclic Pentapeptides Based on Phthaloyl Chloride with Expected Anticancer Activity

Egyptian Journal of Chemistry
Article 10, Volume 63, Issue 5, May 2020, Page 1723-1736  XML PDF (1.58 MB)
Document Type: Original Article
DOI: 10.21608/ejchem.2019.18452.2137
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Authors
Fatma Hassan Mohamed1; Ahmed Shalaby2; Hanan abdelhameid Soliman3; Ahmed Abdelazem4; Marwa Mounier5; Eman Nossierorcid 6; Gaber Moustafa email 1
1Peptide Chemistry Department, National Research Centre, Dokki 12622, Cairo, Egypt
2Peptide Chemistry Department, Chemical Industries Research Division, National Research Centre, Cairo, Egypt
3Biochemistry Department, Faculty of Science, Beni-Suef University, Beni-Suef, Egypt
4Biotechnology and Life Sciences Department, Faculty of Postgraduate Studies for Advanced Sciences, Beni-Suef University, Egypt
5Pharmaceutical and Drug Industries Research Division, Department of Pharmacognosy, National Research Centre, Giza, Egypt
6Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt
Abstract
A series of Nα-phthaloyl bridged cyclic pentapeptide derivatives were synthesized and characterized on the basis of spectral and elemental analyses. A preliminary cytotoxicity evaluation of all novel compounds was carried out against four human cancer cell lines, human lung (A-549), colon (CaCo-2), prostate (PC-3) and breast (MCF-7) cancer cells at 100 μM concentration using MTT growth inhibition assay. Compound 3 gave the highest cytotoxic activity towards the human colon (CaCo-2) cancer cell line (Growth Inhibition = 72.4 %). Further molecular docking of the promising derivative 3 was developed to study its binding mode within the active site of EGFR enzyme. The docking results suggest good fitting through different hydrogen bond interactions with the protein residues to elicit anticancer activity
Keywords
amino acid; linear peptide; cyclic pentapeptide; Nα-phthaloyl-bis-peptides; Cytotoxicity
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