AI Article Synopsis
- The research focuses on developing new drug candidates by increasing structural diversity in medicinal chemistry, specifically through the design of -hydroxyphenyl phosphine borane derivatives.
- The synthesized derivatives showed good stability in water, less hydrophobicity compared to alkanes and silanes, and adequate affinity for lipid membranes, which is important for drug permeability.
- Some of the -hydroxyphenyl phosphine borane derivatives demonstrated significant activity as estrogen receptor agonists, highlighting the potential of this framework in drug discovery.
Article Abstract
Increasing the structural options in medicinal chemistry is a promising approach to develop new drug candidates. In this research, we designed and synthesized a series of -hydroxyphenyl phosphine borane derivatives and investigated their structure-property and structure-activity relationships. The synthesized -phenylphosphine borane derivatives exhibited sufficient stability in aqueous media, weaker hydrophobicity than the corresponding alkanes and silanes, and sufficient affinity for lipid membranes to enable permeability. Several -hydroxyphenyl phosphine borane derivatives exhibited significant estrogen receptor (ER) agonistic activity with superior ligand-lipophilicity efficiency (LLE). The phosphine borane framework appears to be a promising option for structural development in drug discovery studies.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10809333 | PMC |
| http://dx.doi.org/10.1039/d3md00350g | DOI Listing |
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