ISSN : 2663-2187

Structure based design and characterization of the Highly potent and selective Estrogen receptor targeting the Breast cancer cell line

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P.Sivarajani ,R.Ida Malarselvi, C. Ramachandra Raja ,R. Pricilla
» doi: 10.33472/AFJBS.6.9.2024.4463-4477

Abstract

A novel 2-(((3S,5S,6R)-5-methoxy-6-((E)-(phenylimino)tetrahydro-2H-pyran-3-yl)1-diazenyl)phenol (CS-SA) was synthesized to evaluate anticancer activity against MCF-7 breast cancer cell line. The structure of the ligand was confirmed from FT-IR, NMR spectral studies. Estrogen receptor (ER) selective agonists are considered potential therapeutic agents for a variety of pathological conditions, including uterus and breast cancers. Their development is particularly challenging, since differences in the ligand binding cavities of two ER subtypes are minimal. We have carried out rational design of new salicylaldoxime derivatives which display unprecedentedly High-level ER selectivity for this class of compound, both in binding affinity and in cell-based functional assays. An endogenous gene expression assay was used to further characterize the pharmacological action of inhibit proliferation of a breast cancer cell line in-vitro. The new bio-composite is high- quality and high- purity with estrogen receptor ligand binding Domain (PDB ID: 5TOA).

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