Nakamura, Masaharu published the artcileDevelopment of silicon-containing bis-phenol derivatives as androgen receptor antagonists: Selectivity switching by C/Si exchange, SDS of cas: 57044-25-4, the publication is Bioorganic & Medicinal Chemistry (2013), 21(7), 1643-1651, database is CAplus and MEDLINE.
The authors previously reported that bis-phenol derivatives, including LG190178, possess not only vitamin D receptor (VDR) agonistic activity, but also androgen receptor (AR) antagonistic activity. Here, the authors describe the design, synthesis and evaluation of silicon-containing bis-phenol derivatives, with the objective of obtaining increased selectivity toward VDR or AR. The authors found that replacement of the quaternary carbon in the bis-phenol skeleton with silicon increased AR-antagonistic activity and reduced VDR-agonistic activity, i.e., the AR selectivity of the silicon-containing compounds was higher than that of corresponding carbon compounds To the authors’ knowledge, this is the first report of nuclear receptor (NR) selectivity switching by sila-substitution (C/Si exchange). Among the compounds synthesized, AR-selective ligand (I) exhibited more potent anti-androgenic activity (IC50 = 0.072 μM) than hydroxyflutamide, a well-known androgen antagonist (IC50 = 1.4 μM), in SC-3 cell proliferation assay. These results suggest that sila-substitution is a useful approach for structural development of selective AR ligands.
Bioorganic & Medicinal Chemistry published new progress about 57044-25-4. 57044-25-4 belongs to alcohols-buliding-blocks, auxiliary class Epoxides,Chiral,Aliphatic hydrocarbon chain,Alcohol, name is (R)-Oxiran-2-ylmethanol, and the molecular formula is C3H6O2, SDS of cas: 57044-25-4.
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