Volume 33, Issue 227 (12-2023)                   J Mazandaran Univ Med Sci 2023, 33(227): 13-23 | Back to browse issues page

XML Persian Abstract Print

Download citation:
BibTeX | RIS | EndNote | Medlars | ProCite | Reference Manager | RefWorks
Send citation to:

Hariri R, Baeeri M, Mohammadhosseini N, Emami S, Foroumadi A, Barazandeh Tehrani M. Evaluation of Inhibitory Effect and Docking Study of Triazolyl Chromanone Oxime Ether Derivatives on Aromatase Enzyme Effective in Breast Cancer. J Mazandaran Univ Med Sci 2023; 33 (227) :13-23
URL: http://jmums.mazums.ac.ir/article-1-19463-en.html
Abstract:   (385 Views)
Background and purpose: The spread of cancer, coupled with the challenges posed by complex treatments, stands as one of the foremost medical issues in today's world. Researchers consistently strive to identify novel compounds with enhanced efficacy and reduced side effects. Aromatase, a pivotal enzyme in estrogen receptor-positive breast cancer, plays a significant role. Estrogens, crucial for human physiology, particularly in women, contribute to sexual development and reproduction. The adverse effects associated with specific aromatase inhibitors underscore the imperative to discover new inhibitors characterized by higher selectivity, lower toxicity, and improved potency.
Materials and methods: This research is a basic study in which the semi-prepared aromatase kit was used to investigate synthetic compounds, specifically triazolyl chromanone oxime ethers. The most promising compounds were selected and subjected to molecular docking studies based on the inhibition results obtained.
Results: Out of the 40 compounds examined, seven samples exhibiting the most pronounced inhibitory effects were chosen for further scrutiny and IC50 determination. Notably, derivatives 6b and 20b demonstrated the most robust inhibitory effects, with IC50 values of 0.37 and 0.69 μM, respectively. Examining the interactions between these compounds and the aromatase enzyme revealed a significant relationship with the enzyme's active site.
Conclusion: In conclusion, the evaluation of various derivatives containing the triazolyl chromanone oxime ether structure suggests their considerable potential as aromatase enzyme inhibitors. Further exploration involving the design of structures within this category holds the promise of yielding more effective derivatives for inhibiting this enzyme.

Full-Text [PDF 893 kb]   (180 Downloads)    
Type of Study: Research(Original) | Subject: Pharmacy

Add your comments about this article : Your username or Email:

Send email to the article author

Rights and permissions
Creative Commons License This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.

© 2024 CC BY-NC 4.0 | Journal of Mazandaran University of Medical Sciences

Designed & Developed by : Yektaweb