852874-60-3Relevant articles and documents
Selectivity, ligand deconstruction, and cellular activity analysis of a BPTF bromodomain inhibitor
Kirberger, Steven E.,Ycas, Peter D.,Johnson, Jorden A.,Chen, Chen,Ciccone, Michael F.,Woo, Rinette W. L.,Urick, Andrew K.,Zahid, Huda,Shi, Ke,Aihara, Hideki,McAllister, Sean D.,Kashani-Sabet, Mohammed,Shi, Junwei,Dickson, Alex,Dos Santos, Camila O.,Pomerantz, William C. K.
supporting information, p. 2020 - 2027 (2019/02/20)
Bromodomain and PHD finger containing protein transcription factor (BPTF) is an epigenetic protein involved in chromatin remodelling and is a potential anticancer target. The BPTF bromodomain has one reported small molecule inhibitor (AU1, rac-1). Here, advances made on the structure-activity relationship of a BPTF bromodomain ligand are reported using a combination of experimental and molecular dynamics simulations leading to the active enatiomer (S)-1. Additionally, a ligand deconstruction analysis was conducted to characterize important pharmacophores for engaging the BPTF bromodomain. These studies have been enabled by a protein-based fluorine NMR approach, highlighting the versatility of the method for selectivity, ligand deconstruction, and ligand binding. To enable future analysis of biological activity, cell growth analyses in a panel of cancer cell lines were carried out using CRISPR-Cas9 and (S)-1 to identify cell-based model systems that are sensitive to BPTF inhibition.
Fused Ring Compound For Use As Mineralocorticoid Receptor Antagonist
-
Paragraph 0228; 0229, (2013/11/06)
The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4, Cy and n are as presented in the description.
Chiral 3-aminopyrrolidines as a rigid diamino scaffold for organocatalysis and organometallic chemistry
Pouliquen, Mickael,Blanchet, Jerome,Paolis, Michael De,Rema Devi,Rouden, Jacques,Lasne, Marie-Claire,Maddaluno, Jacques
experimental part, p. 1511 - 1521 (2010/11/02)
Over 20 new and easily prepared diamines were screened for the asymmetric Morita-Baylis-Hillman reaction. Chiral non-racemic 3-(N,N-dimethylamino)-1- methylpyrrolidine was found to promote efficiently the reaction of methyl vinyl ketone and substituted benzaldehydes. Enantiomeric excesses up to 73% were reached with electron-deficient benzaldehyde derivatives. After a simple deprotonation, one of these diamines was transformed into a chiral mixed aggregate for the enantioselective synthesis of (R)-1-o-tolylethanol with 76% ee.