721949-01-5Relevant academic research and scientific papers
Synthesis and biological evaluation of spiro-δ-lactones as inhibitors of 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2)
Xu, Kuiying,Wetzel, Marie,Hartmann, Rolf W.,Marchais-Oberwinkler, Sandrine
experimental part, p. 406 - 421 (2012/06/18)
17β-Hydroxysteroid dehydrogenase type 2 (17β-HSD2) catalyzes the oxidation of the potent estradiol (E2) to the less active estrogen estrone (E1). Inhibitors of this enzyme should maintain the local level of E2 in bone tissue when the E2 concentration in t
Novel inhibitors of 17β-hydroxysteroid dehydrogenase type 1: Templates for design
Allan, Gillian M.,Vicker, Nigel,Lawrence, Harshani R.,Tutill, Helena J.,Day, Joanna M.,Huchet, Marion,Ferrandis, Eric,Reed, Michael J.,Purohit, Atul,Potter, Barry V.L.
, p. 4438 - 4456 (2008/09/21)
The 17β-hydroxysteroid dehydrogenases (17β-HSDs) catalyze the interconversion between the oxidized and reduced forms of androgens and estrogens at the 17 position. The 17β-HSD type 1 enzyme (17β-HSD1) catalyzes the reduction of estrone (E1) to estradiol a
6-Aryl-8H-indeno[1,2-d]thiazol-2-ylamines: A1 adenosine receptor agonist allosteric enhancers having improved potency
Chordia, Mahendra D.,Zigler, Molly,Murphree, Lauren J.,Figler, Heidi,Macdonald, Timothy L.,Olsson, Ray A.,Linden, Joel
, p. 5131 - 5139 (2007/10/03)
Allosteric enhancers (AEs) of the A1 adenosine receptor (A 1AR) have potential as drugs for treating neurological, cardiovascular, and renal diseases. This report describes the synthesis and evaluation of a series of 6-aryl-8H-indeno[1,2-d]thiazol-2-ylamines that exhibited AE activity at the A1AR. Palladium-mediated condensation of arylboronic acids with 5-bromoindan-1-one generated arylindanones 2a-aj for iodine-catalyzed condensation with thiourea, generating 2-aminothiazolium salts 3a-aj. Binding studies using membranes from cells stably expressing human A 1ARs, A2AARs, or A3ARs evaluated AE activity and receptor subtype selectivity. The EC50 of the AE activities of compounds 3m-o, 3x, and 3ae were 2.2, 1.5, 0.9, 1.0, and 3.0 μM, respectively, substantially lower than that of the well characterized 2-amino-3-aroylthiophene (PD 81,723), >10 μM. The new compounds also have substantially higher maximal AE activity. These compounds had no AE activity at the A2AAR and only minimal activity at the A3AR. 2005 American Chemical Society.
