Synthesis, In vitro and In silico Studies of Novel Bis‐triazolopyridopyrimidines from Curcumin Analogues as Potential Aromatase Agents

Breast cancer remains a major global health issue, particularly affecting women and contributing significantly to mortality rates. Current treatments for estrogen receptor‐positive breast cancers, such as aromatase inhibitors, are effective but often come with side effects and resistance issues. Thi...

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Published inChemistry & biodiversity Vol. 21; no. 8; pp. e202400701 - n/a
Main Authors Gomha, Sobhi M., El‐Sayed, Abdel‐Aziz A. A., Zaki, Magdi E. A., Alrehaily, Abdulwahed, Elbadawy, Hossein M., Al‐Shahri, Ahmad bin Ali, Alsenani, Saleh Rashed, Abouzied, Amr S.
Format Journal Article
LanguageEnglish
Published Switzerland Wiley Subscription Services, Inc 01.08.2024
Subjects
anticancer activity
Aromatase
Breast cancer
Curcumin
Effectiveness
Estrogen receptors
Estrogens
Global health
hydrazonyl halides
Inhibitors
Line spectra
Medical innovations
Molecular docking
NMR
Nuclear magnetic resonance
Pharmacology
Public health
Pyridopyrimidines
Side effects
Tumor cell lines
Pyridopyrimidines
molecular docking
anticancer activity
aromatase
hydrazonyl halides
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Summary:Breast cancer remains a major global health issue, particularly affecting women and contributing significantly to mortality rates. Current treatments for estrogen receptor‐positive breast cancers, such as aromatase inhibitors, are effective but often come with side effects and resistance issues. This study addresses these gaps by targeting aromatase, an enzyme crucial for estrogen synthesis, which plays a pivotal role in breast cancer progression. The innovative approach involves synthesizing novel bis‐triazolopyridopyrimidines, designed to leverage the combined pharmacological benefits of pyridopyrimidine and 1,2,4‐triazole structures, known for their potent aromatase inhibition and anti‐cancer properties. These compounds were synthesized and characterized using 1H‐NMR, 13C‐NMR, and MS spectral analyses, and their anticancer efficacy was evaluated through MTT assays against MCF‐7 breast cancer cell lines in vitro. Molecular docking analyses revealed strong binding energies with aromatase, particularly for compounds 5 b, 5 c, 10 a, and 10 b, indicating their potential as effective aromatase inhibitors. The study highlights these compounds as promising candidates for further development as therapeutic agents against breast cancer.
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ISSN:1612-1872
1612-1880
1612-1880
DOI:10.1002/cbdv.202400701