Synthesis of New 1,2,3-Triazole-Based Compounds of Potential Anti-Breast Cancer Activity Targeting Aromatase Enzyme Inhibition
Syam, Y., EL-Hggar, R., Anwar, M., Hisham, A., Nosseir, O., Zaghary, W. (2023). Synthesis of New 1,2,3-Triazole-Based Compounds of Potential Anti-Breast Cancer Activity Targeting Aromatase Enzyme Inhibition. EKB Journal Management System, 66(10), 93-106. doi: 10.21608/ejchem.2023.179241.7278
Yasmin M. Syam; Radwan EL-Hggar; Manal M. Anwar; Alaa H. Hisham; Ola Nosseir; Wafaa A. Zaghary. "Synthesis of New 1,2,3-Triazole-Based Compounds of Potential Anti-Breast Cancer Activity Targeting Aromatase Enzyme Inhibition". EKB Journal Management System, 66, 10, 2023, 93-106. doi: 10.21608/ejchem.2023.179241.7278
Syam, Y., EL-Hggar, R., Anwar, M., Hisham, A., Nosseir, O., Zaghary, W. (2023). 'Synthesis of New 1,2,3-Triazole-Based Compounds of Potential Anti-Breast Cancer Activity Targeting Aromatase Enzyme Inhibition', EKB Journal Management System, 66(10), pp. 93-106. doi: 10.21608/ejchem.2023.179241.7278
Syam, Y., EL-Hggar, R., Anwar, M., Hisham, A., Nosseir, O., Zaghary, W. Synthesis of New 1,2,3-Triazole-Based Compounds of Potential Anti-Breast Cancer Activity Targeting Aromatase Enzyme Inhibition. EKB Journal Management System, 2023; 66(10): 93-106. doi: 10.21608/ejchem.2023.179241.7278

Synthesis of New 1,2,3-Triazole-Based Compounds of Potential Anti-Breast Cancer Activity Targeting Aromatase Enzyme Inhibition

Egyptian Journal of Chemistry
Volume 66, Issue 10, October 2023, Page 93-106  XML PDF (594.46 K)
Document Type: Original Article
DOI: 10.21608/ejchem.2023.179241.7278
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Authors
Yasmin M. Syam email 1; Radwan EL-Hggarorcid 2; Manal M. Anwar3; Alaa H. Hisham2; Ola Nosseir4; Wafaa A. Zaghary5
1Department of Therapeutic Chemistry, National Research Centre, Dokki, Cairo, Egypt
2Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Ain Helwan, 11795, Cairo, Egypt.
3Therapeutic Chemistry Department, National Research Centre, Cairo, Egypt.
4Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Ain Helwan, 11795, Cairo, Egypt
5Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, P.O. Box 11795, Cairo, Egypt
Abstract
Depriving the estrogen in the body by inhibiting the aromatase enzyme is thought to be one of the most effective pathways for preventing and treating breast cancer. This study deals with the synthesis of new derivatives bearing a 4-bromophenyl-5-methyl-1,2,3-triazole scaffold hybridized with various heterocyclic rings of reported aromatase inhibition activity such as pyridine, pyrimidine, and pyrazole 4-14, aiming to gain new potent antiproliferative molecules against breast cancer via inhibition of the aromatase enzyme. The cytotoxic activity of the target compounds was evaluated against breast cancer (MCF-7) as well as the normal cell line (WI-38). The derivatives 5b, 5c and 10 were the most promising analogues with a high safety margin against WI38. The latter derivatives were also assessed as aromatase inhibitors and were also subjected to molecular docking studies to determine their potential.
Keywords
1; 2; 3-triazole; breast cancer; aromatase inhibitors; molecular docking; cytotoxicity
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