15862-46-1Relevant articles and documents
Optimization of a Fragment-Based Screening Hit toward Potent DOT1L Inhibitors Interacting in an Induced Binding Pocket
Scheufler, Clemens,M?bitz, Henrik,Gaul, Christoph,Ragot, Christian,Be, Céline,Fernández, César,Beyer, Kim S.,Tiedt, Ralph,Stauffer, Frédéric
, p. 730 - 734 (2016)
Mixed lineage leukemia (MLL) gene rearrangement induces leukemic transformation by ectopic recruitment of disruptor of telomeric silencing 1-like protein (DOT1L), a lysine histone methyltransferase, leading to local hypermethylation of H3K79 and misexpression of genes (including HoxA), which drive the leukemic phenotype. A weak fragment-based screening hit identified by SPR was cocrystallized with DOT1L and optimized using structure-based ligand optimization to yield compound 8 (IC50 = 14 nM). This series of inhibitors is structurally not related to cofactor SAM and is not interacting within the SAM binding pocket but induces a pocket adjacent to the SAM binding site.
A universal acetyl-aminopyridine boric acid frequency alcohol ester preparation method
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Paragraph 0035; 0036, (2017/08/25)
The invention belongs to the field of organic compound synthesis and provides a preparation method of commonly used acetamidopyridine boronic acid pinacol ester. The preparation method comprises the following steps: 1. with halogenated aminopyridine as a starting material, reacting with acetic anhydride in dichloromethane to obtain halogenated acetamidopyridine; and 2. with dioxane as a solvent, mixing the halogenated acetamidopyridine, potassium acetate and bis(pinacolato)diboron under the protection of nitrogen and adding a catalyst ferrocene palladium chloride to react at 60-100 DEG C for 18-24 hours, thus generating the acetamidopyridine boronic acid pinacol ester. The raw materials are convenient to directly purchase from the markets. The preparation method is simple, is convenient to operate, is high in yield and is convenient for industrial production.
Silica-supported boric acid catalyzed synthesis of dihydropyrimidin-2-ones, bis(indolyl)methanes, esters and amides
Kumar, Vishal,Singh, Chitra,Sharma, Upendra,Verma, Praveen K.,Singh, Bikram,Kumar, Neeraj
, p. 83 - 89 (2014/02/14)
Silica-supported boric acid (H3BO3-SiO2) has been established as a green, efficient and recyclable catalyst for the synthesis of dihydropyrimidin-2-ones, bis(indolyl)methanes, and acetylation of alcohols, phenols, amines and thiols under solvent free conditions. The main features of the present method include clean reaction, mild conditions, low loading of environment friendly catalyst and easy workup procedure. The catalyst can be recycled at least five times without any significant loss in activity.