Design and synthesis of 3-benzylaminocoumarin-7- O- sulfamate derivatives as steroid sulfatase inhibitors
Bioorganic Chemistry, ISSN: 0045-2068, Vol: 96, Page: 103618
2020
- 14Citations
- 23Captures
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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
- Citations14
- Citation Indexes14
- 14
- CrossRef3
- Captures23
- Readers23
- 23
Article Description
Steroid sulfatase (STS) is a sulfatase enzyme that catalyzes the conversion of sulfated steroid precursors to free steroid. The inhibition of STS could abate estrogenic steroids that stimulate the proliferation and development of breast cancer, and therefore STS is a potential target for adjuvant endocrine therapy. In this study, a series of 3-benzylaminocoumarin-7- O -sulfamate derivatives targeting STS were designed and synthesized. Structure-relationship activities (SAR) analysis revealed that attachment of a benzylamino group at the 3-position of coumarin improved inhibitory activity. Compound 3j was found to have the highest inhibition activity against human placenta isolated STS (IC 50 0.13 μM) and MCF-7 cell lines (IC 50 1.35 µM). Kinetic studies found compound 3j to be an irreversible inhibitor of STS, with K I and k inact value of 86.9 nM and 158.7 min −1, respectively.
Bibliographic Details
http://www.sciencedirect.com/science/article/pii/S0045206819320772; http://dx.doi.org/10.1016/j.bioorg.2020.103618; http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85079181535&origin=inward; http://www.ncbi.nlm.nih.gov/pubmed/32059152; https://linkinghub.elsevier.com/retrieve/pii/S0045206819320772; https://dx.doi.org/10.1016/j.bioorg.2020.103618
Elsevier BV
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