Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317
Bioorganic & Medicinal Chemistry Letters, ISSN: 0960-894X, Vol: 26, Issue: 7, Page: 1817-1820
2016
- 16Citations
- 11Captures
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
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Metrics Details
- Citations16
- Citation Indexes16
- 16
- CrossRef9
- Captures11
- Readers11
- 11
Article Description
We report the design, synthesis, and physicochemical/biological evaluation of novel silanol derivative 6 (sila-T) as a silanol analog of multi-target nuclear receptor modulator T0901317 ( 5 ). Compound 6 showed intermediate hydrophobicity between the corresponding alcohol 13 and perfluoroalcohol 5. While 5 exhibited potent activities toward liver X receptor α and β, farnesoid X receptor, pregnane X receptor (PXR) and retinoic acid receptor-related orphan receptor (ROR)γ, silanol 6 exhibited activity only toward PXR and RORs. Incorporation of silanol instead of perfluoroalcohol is a promising option for developing novel target-selective, biologically active compounds.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0960894X16301433; http://dx.doi.org/10.1016/j.bmcl.2016.02.031; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84978932837&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/26905831; https://linkinghub.elsevier.com/retrieve/pii/S0960894X16301433; https://dx.doi.org/10.1016/j.bmcl.2016.02.031
Elsevier BV
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