2‐Difluoromethoxy‐Substituted Estratriene Sulfamates: Synthesis, Antiproliferative SAR, Antitubulin Activity, and Steroid Sulfatase Inhibition
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DOI: 10.1002/cmdc.202200408
Abstract: 2‐Difluoromethoxyestratriene derivatives were designed to improve potency and in vivo stability of the drug candidate 2‐methoxyestradiol (2ME2). Compound evaluation in vitro against the proliferation of MCF‐7 and MDA MB‐231 breast cancer cells, as inhibitors of tubulin polymerisation… read more here.
Keywords: difluoromethoxy substituted; steroid sulfatase; inhibition; substituted estratriene ... See more keywords
Sex-Dependent Role of Estrogen Sulfotransferase and Steroid Sulfatase in Metabolic Homeostasis.
Sign Up to like & getrecommendations! Published in 2017 at "Advances in experimental medicine and biology"
DOI: 10.1007/978-3-319-70178-3_21
Abstract: Sulfonation and desulfation are two opposing processes that represent an important layer of regulation of estrogenic activity via ligand supplies. Enzymatic activities of families of enzymes, known as sulfotransferases and sulfatases, lead to structural and… read more here.
Keywords: metabolic homeostasis; estrogen; estrogen sulfotransferase; steroid sulfatase ... See more keywords
Design and synthesis of 3-benzylaminocoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.103618
Abstract: 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,… read more here.
Keywords: design synthesis; sulfamate derivatives; benzylaminocoumarin sulfamate; steroid sulfatase ... See more keywords
Dual Targeting of Steroid Sulfatase and 17β-Hydroxysteroid Dehydrogenase Type 1 by a Novel Drug-Prodrug Approach: A Potential Therapeutic Option for the Treatment of Endometriosis.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00589
Abstract: A novel approach for the dual inhibition of steroid sulfatase (STS) and 17β-hydroxysteroid dehydrogenase type 1(17β HSD1) by a single drug was explored, starting from in-house 17β HSD1 inhibitors via masking their phenolic OH group… read more here.
Keywords: drug prodrug; steroid sulfatase; hydroxysteroid dehydrogenase; drug ... See more keywords
Steroid hormones sulfatase inactivation extends lifespan and ameliorates age-related diseases
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DOI: 10.1038/s41467-020-20269-y
Abstract: Aging and fertility are two interconnected processes. From invertebrates to mammals, absence of the germline increases longevity. Here we show that loss of function of sul-2 , the Caenorhabditis elegans steroid sulfatase (STS), raises the… read more here.
Keywords: longevity; hormones sulfatase; sulfatase inactivation; related diseases ... See more keywords
X-linked ichthyosis associated with psychosis and behavioral abnormalities: a case report
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DOI: 10.1186/s13256-017-1420-2
Abstract: BackgroundX-linked ichthyosis is a dermatological condition caused by deficiency for the enzyme steroid sulfatase. Previously, X-linked ichthyosis/steroid sulfatase deficiency has been associated with developmental and neurological phenotypes. Here, we show for the first time, that… read more here.
Keywords: case; linked ichthyosis; report; steroid sulfatase ... See more keywords
Design, structure-activity relationships, and enzyme kinetic studies of tricyclic and tetracyclic coumarin-based sulfamates as steroid sulfatase inhibitors.
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DOI: 10.2139/ssrn.4329376
Abstract: Inhibition of steroid sulfatase (STS) decreases estrogen production and thus, suppresses tumor proliferation. Inspired by irosustat, the first STS inhibitor in clinical trials, we explored twenty-one tricyclic and tetra-heterocyclic coumarin-based derivatives. Their STS enzyme kinetic… read more here.
Keywords: steroid sulfatase; design structure; structure activity; enzyme kinetic ... See more keywords