Anticancer Activities of Newly Synthesized Chiral Macrocyclic Heptapeptide Candidates.

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

doi:10.3390/molecules25051253

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.

Highlights

Cancer is the second most common causative disease threatening human life
In the present work we report the synthesis of newly macrocyclic pyridoheptapeptide derivatives
2–6 using Nα-dipicolinoyl-bis[dipeptide-carboxylic acid] (1a–c) [29] as starting material, and they were screened as anticancer agents

Summary

Introduction

Cancer is the second most common causative disease threatening human life. Researchers have focused their works on developing successful therapeutic drugs capable of treating different cancer cells. Most research has been focused on developing early-stage cancer-treating drugs, which have received better attention in comparison to drugs used to treat late cancer phases [1]. Besides naturally obtained preparations; i.e., plant-derived extracts and microbially produced antibiotics, chemical synthesis is still used as a traditional method for obtaining potential anticancer drugs. Among chemically synthesized pharmaceutical drugs, macrocyclic compounds with a ring of 12 or more atoms [2] are generally favored for synthesizing potential anticancer derivatives, mainly in the chemical, biological, and medical sectors [3,4,5]. Macrocyclic derivatives include peptideand non-peptide-derived compounds, synthesized peptides, and macrocyclic derivatives [6]

Methods

Results

Conclusion