Fluorescent Azasteroids through Ultrasound Assisted Cycloaddition Reactions [PDF]
We report here the synthesis and optical spectral properties of several new azasteroid derivatives. The formation of these compounds was explained based on the most probable mechanism.
Costel Moldoveanu +2 more
doaj +5 more sources
5-alpha-reductase type I (SRD5A1) is up-regulated in non-small cell lung cancer but does not impact proliferation, cell cycle distribution or apoptosis [PDF]
Background Non-small cell lung cancer (NSCLC) is one of the most frequent malignancies and has a high mortality rate due to late detection and lack of efficient treatments.
Kapp Friedrich G +4 more
doaj +5 more sources
The 5 alpha-reductase isozyme family: a review of basic biology and their role in human diseases. [PDF]
Despite the discovery of 5 alpha-reduction as an enzymatic step in steroid metabolism in 1951, and the discovery that dihydrotestosterone is more potent than testosterone in 1968, the significance of 5 alpha-reduced steroids in human diseases was not ...
Azzouni F, Godoy A, Li Y, Mohler J.
europepmc +4 more sources
Novel 4-Azapregnene Derivatives as Potential Anticancer Agents: Synthesis, Antiproliferative Activity and Molecular Docking Studies [PDF]
A series of novel 21E-arylidene-4-azapregn-5-ene steroids has been successfully designed, synthesized and structurally characterized, and their antiproliferative activity was evaluated in four different cell lines.
Vanessa Brito +4 more
doaj +2 more sources
Inhibition of Phytosterol Biosynthesis by Azasterols [PDF]
Inhibitors of enzymes in essential cellular pathways are potent probes to decipher intricate physiological functions of biomolecules. The analysis of Arabidopsis thaliana sterol profiles upon treatment with a series of azasterols reveals a specific in ...
Sylvain Darnet +5 more
doaj +2 more sources
Pharmacologic properties and inhibitory activity of 6-azasteroids against Mycobacterium leprae in vivo and in vitro [PDF]
Although the current multidrug therapy (MDT) for leprosy is very successful, the long treatment duration and the emergence of antibiotic-resistant strains demand for new alternative drugs.
Thabatta L. S. A. Rosa +13 more
doaj +2 more sources
Steroid diversification by multicomponent reactions. [PDF]
Reports on structural diversification of steroids by means of multicomponent reactions (MCRs) have significantly increased over the last decade. This review covers the most relevant strategies dealing with the use of steroidal substrates in MCRs ...
Reguera L +3 more
europepmc +3 more sources
Synthesis of 5-azaandrostane-3β, 17β-diol protected at the 17-hydroxyl group [PDF]
In the present paper, the preparation of 3β-hydroxy-17β-dimethyl-tert-butylsilyloxy- 5-azaandrostane (15) in fourteen steps is described. B-nor-17-oxoandrost- 5-en-3β-yl acetate (1)1,2 was used as the starting material, which was transformed to the key ...
Pavlović Vladimir D. +4 more
doaj +5 more sources
SAR Analysis of Small Molecules Interfering with Energy-Metabolism in Mycobacterium tuberculosis. [PDF]
Tuberculosis remains the world’s top infectious killer: it caused a total of 1.5 million deaths and 10 million people fell ill with TB in 2018. Thanks to TB diagnosis and treatment, mortality has been falling in recent years, with an estimated 58 million
Appetecchia F +4 more
europepmc +3 more sources
19-Nor-10-azasteroids, a New Class of Steroid 5α-Reductase Inhibitors. 2. X-ray Structure, Molecular Modeling, Conformational Analysis of 19-Nor-10-azasteroids and Comparison with 4-Azasteroids and 6-Azasteroids [PDF]
19-Nor-10-azasteroids are a new class of 5 alpha-reductase inhibitors whose activity depends on the presence of the bridgehead N-10 atom conjugated with the 4-en-3-one moiety in the A ring. The X-ray structure of 19-nor-10-azasteroid 1 has been determined and it is compared with the X-ray structure of testosterone. A complete conformational analysis of
Antonio Guarna +2 more
exaly +6 more sources

