1759-35-9Relevant articles and documents
Investigations on 16-Arylideno Steroids as a New Class of Neuroprotective Agents for the Treatment of Alzheimer’s and Parkinson’s Diseases
Singh, Ranjit,Bansal, Ranju
, p. 186 - 200 (2017)
Neuroinflammatory mechanisms mediated by activated glial and cytokines (TNF-α, IL-1β) might contribute to neuronal degeneration leading to Alzheimer’s (AD) and Parkinson’s disease (PD). Lipopolysaccharide (LPS) is an inflammogen derived from the cell wall of Gram-negative bacteria, which promotes neuroinflammation and subsequent neurodegeneration. Dehydroepiandrosterone (DHEA) and testosterone have been reported as neuroprotective steroids useful for the treatment of various neurodegenerative disorders. In the present study, several 16-arylidene steroidal derivatives have been evaluated as neuroprotective agents in LPS-treated animal models. It was observed that 16-arylidene steroidal derivatives 1a-d and 6a-h considerably improve LPS-induced learning, memory, and movement deficits in animal models. Biochemical estimations of brain serum of treated animals revealed suppression of oxidative and nitrosative stress, acetylcholinesterase activity, and reduction in TNF-α levels, which were induced through LPS mediated neuroinflammatory mechanisms leading to neurodegeneration of brain. Of all the steroidal derivatives, 16-(4-pyridylidene) steroid 1c and its 4-aza analogue 6c were found to be the most active neuroprotective agents and produced effects comparable to standard drug celecoxib at a much lower dose and better than dexamethasone at the same dose in terms of behavioral, biochemical, and molecular aspects.
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-Selective Androgen Receptor Modulators (SARMs)
Mitchell, Helen J.,Dankulich, William P.,Hartman, George D.,Prueksaritanont, Thomayant,Schmidt, Azriel,Vogel, Robert L.,Bai, Chang,McElwee-Witmer, Sheila,Zhang, Hai Z.,Chen, Fang,Leu, Chih-Tai,Kimmel, Donald B.,Ray, William J.,Nantermet, Pascale,Gentile, Michael A.,Duggan, Mark E.,Meissner, Robert S.
scheme or table, p. 4578 - 4581 (2010/03/02)
A novel series of 16-substituted-4-azasteroids has been identified as potential tissue-selective androgen receptor modulators. These ligands display potenthARbinding and agonist activity, low virilizing potential, and good pharmacokinetic profiles in dogs
Novel partial synthetic approaches to replace carbons 2,3,4 of steroids. A methodology to label testosterone and progesterone with 13C in the steroid A ring. Part 1
De Avellar, Isa G.J.,Vierhapper, Friedrich W.
, p. 9957 - 9965 (2007/10/03)
A synthetic route to replace A ring carbon atoms 2, 3 and 4 of steroid hormones is described. Readily available testosterone propionate or progesterone, respectively, are degraded to the corresponding 10-formyl-5-oxo-des-A intermediates, in a first stage to the preparation of 2,3,4-(13C3)-labeled steroids. (C) 2000 Elsevier Science Ltd.
