Novel steroid sulfatase inhibitors based on N ‐thiophosphorylated 3‐(4‐aminophenyl)‐coumarin‐7‐O‐sulfamates

2019 ◽  
Vol 80 (6) ◽  
pp. 857-866 ◽  
Author(s):  
Mateusz Daśko ◽  
Sebastian Demkowicz ◽  
Karol Biernacki ◽  
Amira Harrous ◽  
Janusz Rachon ◽  
...  
Keyword(s):  
Steroid Sulfatase ◽  
Coumarin 7

Synthesis and steroid sulfatase inhibitory activities of N-phosphorylated 3-(4-aminophenyl)-coumarin-7-O-sulfamates

MedChemComm ◽  
2016 ◽  
Vol 7 (6) ◽  
pp. 1146-1150 ◽  
Author(s):  
Mateusz Daśko ◽  
Maciej Masłyk ◽  
Konrad Kubiński ◽  
Justyna Aszyk ◽  
Janusz Rachon ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Steroid Sulfatase ◽  
Coumarin 7 ◽  
Inhibitory Activities ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

In the present work, we report convenient methods for the synthesis and biological evaluation of N-phosphorylated derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as potential steroid sulfatase (STS) inhibitors.

ChemInform Abstract: Synthesis and Antimicrobial Activity of Coumarin 7-Substituted Cephalosporins and Sulfones.

ChemInform ◽  
2010 ◽  
Vol 29 (50) ◽  
pp. no-no
Author(s):  
L. BONSIGNORE ◽  
F. COTTIGLIA ◽  
H. ELKHAILI ◽  
F. JEHL ◽  
S. M. LAVAGNA ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Coumarin 7

scholarly journals Steroid hormones sulfatase inactivation extends lifespan and ameliorates age-related diseases

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Mercedes M. Pérez-Jiménez ◽  
José M. Monje-Moreno ◽  
Ana María Brokate-Llanos ◽  
Mónica Venegas-Calerón ◽  
Alicia Sánchez-García ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Caenorhabditis Elegans ◽  
Protein Aggregation ◽  
Steroid Hormones ◽  
Sensory Neurons ◽  
Environmental Cues ◽  
Steroid Sulfatase ◽  
Loss Of Function ◽  
C Elegans ◽  
Age Related

AbstractAging 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 pool of sulfated steroid hormones, increases longevity and ameliorates protein aggregation diseases. This increased longevity requires factors involved in germline-mediated longevity (daf-16, daf-12, kri-1, tcer-1 and daf-36 genes) although sul-2 mutations do not affect fertility. Interestingly, sul-2 is only expressed in sensory neurons, suggesting a regulation of sulfated hormones state by environmental cues. Treatment with the specific STS inhibitor STX64, as well as with testosterone-derived sulfated hormones reproduces the longevity phenotype of sul-2 mutants. Remarkably, those treatments ameliorate protein aggregation diseases in C. elegans, and STX64 also Alzheimer’s disease in a mammalian model. These results open the possibility of reallocating steroid sulfatase inhibitors or derivates for the treatment of aging and aging related diseases.

scholarly journals Structure-Activity Relationship for the First-in-Class Clinical Steroid Sulfatase Inhibitor Irosustat (STX64, BN83495)

ChemMedChem ◽  
2011 ◽  
Vol 6 (11) ◽  
pp. 2019-2034 ◽  
Author(s):  
L. W. Lawrence Woo ◽  
Dharshini Ganeshapillai ◽  
Mark P. Thomas ◽  
Oliver B. Sutcliffe ◽  
Bindu Malini ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Steroid Sulfatase ◽  
Structure Activity

Synthesis, in vitro and in vivo activity of benzophenone-based inhibitors of steroid sulfatase

2004 ◽  
Vol 12 (10) ◽  
pp. 2759-2772 ◽  
Author(s):  
Hatem A.M Hejaz ◽  
L.W.Lawrence Woo ◽  
Atul Purohit ◽  
Michael J Reed ◽  
Barry V.L Potter
Keyword(s):  
Steroid Sulfatase
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