15360-53-9Relevant articles and documents
Nickel-Catalyzed Intramolecular Decarbonylative Coupling of Aryl Selenol Esters
Bai, Jin-Hua,Qi, Xiu-Juan,Sun, Wei,Yu, Tian-Yang,Xu, Peng-Fei
supporting information, p. 2084 - 2088 (2021/03/01)
This report describes a method for Ni-catalyzed intramolecular decarbonylative coupling, which enables the conversion of areneselenol esters to diaryl selenides. The inexpensive and readily available catalyst can be employed under mild reaction conditions for the construction of structurally diverse diaryl selenides, including heterocyclic and natural product derivatives. (Figure presented.).
METHODS OF ACTIVATING MICROGLIAL CELLS
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Page/Page column 50; 52, (2020/02/23)
The present disclosure provides methods of using compositions that inhibit SH2-containing inositol 5'-phosphatases (SHIPs) for activating microglial cells, as well as methods for using such compositions for treatment or ameliorating of neurodegenerative disorders in a subject.
HUMAN GHRELIN O-ACYL TRANSFERASE INHIBITORS
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Sheet 10, (2018/03/09)
A class of cyanosteroid compounds that efficiently inhibit ghrelin acylation by ghrelin O-acyltransferase. The compounds have a steroid scaffold with α,β-unsaturated ketone in the A ring position such an a-cyanoenone. Exemplary compounds include (5S,8S,9S,10S, 13S,14S)-10,13-dimethyl-3-oxo-4,5,6,7,8,9,10,11,12,13,14,15,16,17- tetradecahydro-3H-cyclopenta[a]phenanthrene-2-carbonitrile.
AMPHIPHILIC COMPOUNDS WITH NEUROPROTECTIVE PROPERTIES
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Page/Page column 36, (2016/03/22)
The present invention provides amphiphilic compounds with tetradecahydrophenanthrene skeleton and their enantiomers, exhibiting neuroprotective effects, their use as medicaments for treating neuropsychiatric disorders associated with an imbalance in glutamatergic neurotransmitter system, such as ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, post-traumatic stress disorder and diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addiction, multiple sclerosis, epilepsy, glioma, and a pharmaceutical composition containing said compound.
A New Class of Potent N-Methyl- d -Aspartate Receptor Inhibitors: Sulfated Neuroactive Steroids with Lipophilic D-Ring Modifications
Kudova, Eva,Chodounska, Hana,Slavikova, Barbora,Budesinsky, Milos,Nekardova, Michaela,Vyklicky, Vojtech,Krausova, Barbora,Svehla, Pavel,Vyklicky, Ladislav
, p. 5950 - 5966 (2015/08/24)
N-Methyl-d-aspartate receptors (NMDARs) are glutamate-gated ion channels that play a crucial role in excitatory synaptic transmission. However, the overactivation of NMDARs can lead to excitotoxic cell damage/death, and as such, they play a role in numerous neuropathological conditions. The activity of NMDARs is known to be influenced by a wide variety of allosteric modulators, including neurosteroids, which in turn makes them promising therapeutic targets. In this study, we describe a new class of neurosteroid analogues which possess structural modifications in the steroid D-ring region. These analogues were tested on recombinant GluN1/GluN2B receptors to evaluate the structure-activity relationship. Our results demonstrate that there is a strong correlation between this new structural feature and the in vitro activity, as all tested compounds were evaluated as more potent inhibitors of NMDA-induced currents (IC50 values varying from 90 nM to 5.4 μM) than the known endogeneous neurosteroid-pregnanolone sulfate (IC50 = 24.6 μM).
SHIP INHIBITION TO COMBAT OBESITY
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Paragraph 00194, (2015/01/16)
The present invention relates to the use of SHIP1 inhibitors and pan-SHIP1/2 inhibitors in various methods, including, without limitation: (i) a method to treat obesity or reduce body fat of an obese subject; (ii) a method to limit bone development in a subject suffering from an osteopetrotic or sclerotic disease; (iii) a method to treat or prevent diabetes; (iv) a method to reduce glucose intolerance or insulin resistance; and (v) a method to lower cholesterol.
Androstanes with modified carbon skeletons
Norden, Sascha,Bender, Matthias,Rullkoetter, Juergen,Christoffers, Jens
experimental part, p. 4543 - 4550 (2011/09/16)
Four sterane hydrocarbons were prepared for comparisonwith fossil organic biomarkers in geological samples from Oman. 17ss-Methylestrane was prepared in six steps (36% overall yield) from estrone methyl ether. Key steps of this sequence were a Wittig olefination and Birch reduction of the A-ring. 17ss-Methylandrostane was obtained in four steps (85% overall yield) from trans-androsterone by four functional group interconverting reactions, including aWittig olefination. 17ss-Methyl-and 2α-methyl-A-nor-5α- androstanes (14 and 15% overall yields, respectively) were also prepared from trans-androsterone. Key steps were the thallium trinitrate mediated ring contractions of A-ring ketones to A-nor-2-carboxylic acids. Defunctionalization in the four syntheses was achieved by catalytic hydrogenation, Huang-Minlon reduction, Barton decarboxylation, and Bu3SnH-mediated reduction of a chloromethyl group, respectively.
SHIP INHIBITORS AND USES THEREOF
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Page/Page column 31-33, (2011/10/31)
The present invention relates to SHIP inhibitor compounds and methods for using these compounds. In particular, the present invention discloses the following methods: (i) a method of treating graft versus host disease in a subject; (ii) a method of inhibiting a SHIP1 protein in a cell; (iii) a method of selectively inhibiting a SHIP1 protein in a cell; (iv) a method for treating or preventing graft-versus-host disease (GVHD) in a recipient of an organ or tissue transplant; (v) a method of modulating SHIP activity in a cell expressing SHIP1 or SHIP2; (vi) a method of ex vivo or in vitro treatment of transplants; (vii) a method of inhibiting tumor growth and metastasis in a subject; (viii) a method of treating a hematologic malignancy in a subject; (ix) a method of inducing apoptosis of multiple myeloma cells; (x) a method of treating multiple myeloma in a subject; (xi) a method of inhibiting the proliferation of a human breast cancer cell; and (xii) a method of treating breast cancer in a subject.
Novel and efficient synthesis and antifungal evaluation of 2,3-functionalized cholestane and androstane derivatives
Jursic, Branko S.,Upadhyay, Sunil Kumar,Creech, Clinton C.,Neumann, Donna M.
supporting information; experimental part, p. 7372 - 7375 (2011/02/23)
Synthetic modifications of cholesterol and other traditional steroid molecules have become a promising area for the exploration and development of novel antifungal agents, especially with respect to the development of fatty-acid esters of steroids. In addition, 2,3-functionalized steroids are also compounds with potentially interesting biological properties and proper functionalization of 2,3-steroids can lead to the development of efficient syntheses of building blocks for novel fatty-acid esters of steroids. In this Letter, we outline a novel and efficient approach to the synthesis of 2,3-functionalized cholestane and androstane derivatives and present their promising preliminary antifungal activities against a number of fungal species.
One-pot reductive cleavage of exo-olefin to methylene with a mild ozonolysis-Clemmensen reduction sequence
Xu, Shu,Toyama, Takayuki,Nakamura, Jun,Arimoto, Hirokazu
scheme or table, p. 4534 - 4537 (2010/10/02)
A one-pot exo-olefin reductive cleavage was for the first time developed. The reaction could proceed under a mild condition avoiding the use of hazardous and expensive reagents. Meanwhile, a TMSCl-mediated Clemmensen reduction in alcoholic solvent was also examined.
