17099-07-9Relevant academic research and scientific papers
Development of novel vitamin D receptor-coactivator inhibitors
Sidhu, Preetpal S.,Nassif, Nicholas,McCallum, Megan M.,Teske, Kelly,Feleke, Belaynesh,Yuan, Nina Y.,Nandhikonda, Premchendar,Cook, James M.,Singh, Rakesh K.,Bikle, Daniel D.,Arnold, Leggy A.
supporting information, p. 199 - 204 (2014/03/21)
Nuclear receptor coregulators are master regulators of transcription and selectively interact with the vitamin D receptor (VDR) to modulate cell differentiation, cell proliferation, and calcium homeostasis. Herein, we report the syntheses and evaluation of highly potent and selective VDR-coactivator inhibitors based on a recently identified 3-indolylmethanamine scaffold. The most active compound, PS121912, selectively inhibited VDR-mediated transcription among eight other nuclear receptors tested. PS121912 is also selectively disrupting the binding between VDR and the third nuclear receptor interaction domain of the coactivator SRC2. Genetic studies revealed that PS121912 behaves like a VDR antagonist by repressing 1,25-(OH)2D3 activated gene transcription. In addition, PS121912 induced apoptosis in HL-60.
Synthesis of 4-imino-2H,3H,5H-[1,2,5]thiadiazolidin-1-oxide through cycloaddition reaction of N-sulphinylanilines and N-(α-cyano-α-aryl) -methylanilines
Kaur, Manpreet,Singh, Baldev
, p. 1157 - 1161 (2014/08/05)
Through the normal mode of cycloaddition reaction of N-(α-cyano- α-aryl)-methylanilines (II) onto N-sulphinylanilines (III) has provided 2,3,5-triaryl-4-imino-2H,3H,5H-[1,2,5]thiadiazolidin-1-oxides (IV). The present protocol has advantage of convenient operation to synthesize heterocyclics in good yield.
CANNABINOID RECEPTOR LIGANDS AND USES THEREOF
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Page/Page column 27, (2010/11/26)
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.
Synthesis and reduction of nitrones of 2-chlorobenzaldehyde and their antifungal potential
Matharu, Balbir Kaur,Sharma,Manrao
, p. 917 - 918 (2007/10/03)
Condensation of 2-chlorobenzaldehyde with phenylhydroxylamines resulted in the foripation of C-(2-chlorophenyl)-N-phenylnitrones (1a-6a) which were characterized on the basis of elemental analysis and spectral studies. Sodium borohydride reduction of the nitrones was carried out and the nitrones were screened for their antifungal potential against five phytopathogenic fungi.
Polarographic investigations on azomethines: Benzal-p-chloranilines in alkaline medium and effect of substituents on half-wave potentials
Katiyar, Sarvagya S.,Lalithambika, M.
, p. 961 - 973 (2007/10/02)
Polarographic behavior of twenty-four substituted benzal-p-chloranilines has been investigated in 50percent methanol-water medium in alkaline pH range.The experimental conditions for the study were so designed that no appreciable hydrolysis of the Schiff
