Anticancer Activities of Newly Synthesized Chiral Macrocyclic Heptapeptide Candidates

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 deriv...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2020-03, Vol.25 (5), p.1253
Main Authors: Abo-Ghalia, Mohamed H, Moustafa, Gaber O, Amr, Abd El-Galil E, Naglah, Ahmed M, Elsayed, Elsayed A, Bakheit, Ahmed H
Format: Article
Language:English
Subjects:
3,5-tetrapeptidopyridine
Amino acids
Antineoplastic Agents - pharmacology
Breast cancer
Breast Neoplasms - drug therapy
Cancer therapies
Caustic soda
Cell Line, Tumor
Chemical compounds
Chemical synthesis
Cytotoxicity
Drug Screening Assays, Antitumor - methods
Drugs
Female
Hep G2 Cells
Humans
in vitro anticancer activity
Liver cancer
Liver Neoplasms - drug therapy
Macrocyclic Compounds - pharmacology
macrocyclic heptapeptides
MCF-7 Cells
Molecular Docking Simulation - methods
NMR
Nuclear magnetic resonance
Peptide Fragments - physiology
Peptides
Pharmaceuticals
Pharmacology
Sodium
Structure-Activity Relationship
Toxicity
Tumor cell lines
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Summary: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.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules25051253