Anticancer Activities of Newly Synthesized Chiral Macrocyclic Heptapeptide Candidates

Mohamed H Abo-Ghalia; Gaber O Moustafa; Abd El-Galil E Amr; Ahmed M Naglah; Elsayed A Elsayed; Ahmed H Bakheit

doi:10.3390/molecules25051253

Anticancer Activities of Newly Synthesized Chiral Macrocyclic Heptapeptide Candidates

Molecules. 2020 Mar 10;25(5):1253. doi: 10.3390/molecules25051253.

Authors

Mohamed H Abo-Ghalia¹, Gaber O Moustafa¹, Abd El-Galil E Amr^{2

3}, Ahmed M Naglah^{1

2}, Elsayed A Elsayed^{4

5}, Ahmed H Bakheit^{6

7}

Affiliations

¹ Department of Peptide Chemistry, National Research Centre, Dokki 12622, Cairo, Egypt.
² Pharmaceutical Chemistry Department, Drug Exploration & Development Chair (DEDC), College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
³ Applied Organic Chemistry Department, National Research Centre, Dokki 12622, Cairo, Egypt.
⁴ Bioproducts Research Chair, Zoology Department, Faculty of Science, King Saud University, Riyadh 11451, Saudi Arabia.
⁵ Chemistry of Natural and Microbial Products Department, National Research Centre, Dokki 12622, Cairo, Egypt.
⁶ Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, PO Box 2457, Riyadh 11451, Saudi Arabia.
⁷ Department of Chemistry, Faculty of Science and Technology, El-Neelain University, PO Box 12702, Khartoum 11121, Sudan.

Abstract

As important cancer therapeutic agents, macrocyclic peptides have recently drawn great attention, mainly because they are synthetically accessible and have lower toxicity towards normal cells. In the present work, we synthesized newly macrocyclic pyridoheptapeptide derivatives. The synthesized derivatives were characterized using standard chemical and spectroscopic analytical techniques, and their anticancer activities against human breast and hepatocellular cancer cells were investigated. Results showed that compounds 1a and 1b were the most effective against hepatocellular (HepG2) and breast (MCF-7) cancer cell lines, respectively.

Keywords: 3,5-tetrapeptidopyridine; amino acids; in vitro anticancer activity; macrocyclic heptapeptides.

MeSH terms

Antineoplastic Agents / pharmacology*
Breast Neoplasms / drug therapy
Cell Line, Tumor
Drug Screening Assays, Antitumor / methods
Female
Hep G2 Cells
Humans
Liver Neoplasms / drug therapy
MCF-7 Cells
Macrocyclic Compounds / pharmacology
Molecular Docking Simulation / methods
Peptide Fragments / physiology*
Structure-Activity Relationship

Substances

Antineoplastic Agents
Macrocyclic Compounds
Peptide Fragments

Grants and funding

Researchers Supporting Project (No. RSP-2019/66/King Saud University