69628-97-3

Upstream product

• 52022-77-2 2-(3-nitrophenyl)ethanol 
• 1877-73-2 3-nitro-benzeneacetic acid 
• 98-59-9 p-toluenesulfonyl chloride 

Downstream Products

• 80641-92-5 N-(2-(m-nitrophenyl)ethyl)-1,4-diazabicyclo<2.2.2>octanium tosylate 
• 97351-96-7 3-nitro-N,N-dipropylbenzeneethanamine 
• 402508-77-4 thioacetic acid S-[2-(3-nitrophenyl)ethyl] ester 
• 1214924-42-1 (1S,2S,3R,4R,5R)-3-(2-chloro-5-fluoropyrimidin-4-ylamino)-5-(3-nitrophenethylamino)bicyclo[2.2.1]heptane-2-carboxamide 
• 1214923-96-2 (1R,2S,3R,4R)-3-(2-chloro-5-fluoropyrimidin-4-ylamino)-5-((3-nitrophenethyl-amino)methyl)bicyclo[2.2.1]heptane-2-carboxamide 
• 1214923-85-9 (1S,2S,3S,4S,5R)-3-[(2-chloro-5-fluoropyrimidin-4-yl)amino]-5-{[2-(3-nitrophenyl)ethyl]thio}bicyclo[2.2.1]heptane 
• 1214923-86-0 (1S,2S,3S,4S,5R)-5-{[2-(3-aminophenyl)ethyl]thio}-3-[(2-chloro-5-fluoropyrimidin-4-yl)amino]bicyclo[2.2.1]heptane-2-carboxamide 
• 1257078-41-3 2-(methyl(3-nitrophenethyl)amino)ethanol 
• 1050530-06-7 C₂₆H₂₂N₂O₆ 
• 103544-23-6 3'-<2-(N,N-di-n-propylamino)ethyl>aniline 

Relevant academic research and scientific papers

Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2-EED Interaction

Disruption of EZH2-embryonic ectoderm development (EED) protein-protein interaction (PPI) is a new promising cancer therapeutic strategy. We have previously reported the discovery of astemizole, a small-molecule inhibitor targeting the EZH2-EED PPI. Herein, we report the cocrystal structure of EED in complex with astemizole at 2.15 ?. The structure elucidates the detailed binding mode of astemizole to EED and provides a structure-guided design for the discovery of a novel EZH2-EED interaction inhibitor, DC-PRC2in-01, with an affinityKdof 4.56 μM. DC-PRC2in-01 destabilizes the PRC2 complex, thereby leading to the degradation of PRC2 core proteins and the decrease of global H3K27me3 levels in cancer cells. The proliferation of PRC2-driven lymphomas cells is effectively inhibited, and the cell cycle is arrested in the G0/G1 phase. Together, these data demonstrate that DC-PRC2in-01 could be an effective chemical probe for investigating the PRC2-related physiology and pathology and providing a promising chemical scaffold for further development.

MACROCYCLICS PYRIMIDINES AS AURORA KINASE INHIBITORS

Macrocyclic derivative compounds that inhibit protein kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed kinase activity such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.

PYRIMIDINE INHIBITORS OF KINASE ACTIVITY

The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, wherein G1, R2, R3, R4, R5, n, p, q, Ar1, and Ar2 are defined in the description. The present invention relates also to methods of making said compounds, and compositions comprising said compounds which are useful for inhibiting kinases such as IGF-IR.

Planar chiral azobenzenophanes as chiroptic switches for photon mode reversible reflection color control in induced chiral nematic liquid crystals

In this report, for the first time, a planar chiral photoresponsive compound has been employed in commercially available nematic liquid crystals to achieve phototunable reflection colors. We designed an azobenzenophane compound having conformational restr

Opioid ligands with mixed properties from substituted enantiomeric N-phenethyl-5-phenylmorphans. Synthesis of a -agonist δ-antagonist and δ-inverse agonists

Enantiomeric N-phenethyl-m-hydroxyphenylmorphans with various substituents in the ortho, meta or para positions of the aromatic ring in the phenethylamine side-chain (chloro, hydroxy, methoxy, nitro, methyl), as well as a pyridylethyl and a indolylethyl m

PHENYLALKYL AND PYRIDYLALKYL PIPERAZINE DERIVATIVES

This invention relates to compounds of the formula (1) wherein R1, R3, R4, X1, and X2 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system and other disorders.

Synthesis and evaluation of potent and selective β3 adrenergic receptor agonists containing acylsulfonamide, sulfonylsulfonamide, and sulfonylurea carboxylic acid isosteres

Starting from phenethanolamine aniline leads 3a and 3b, we have identified a series of functionally potent and selective β3 adrenergic receptor (AR) agonists containing acylsulfonamide, sulfonylsulfonamide, or sulfonylurea groups within the ani

General Base Catalysis, Structure-Reactivity interactions, and Merging of Mechanisms for Elimination Reactions of (2-Arylethyl)quinuclidinium Ions

Structure-reactivity parameters and interaction coefficients are reported for elimination reactions of N-(2-arylethyl)quinuclidinium ions and for 2-arylethyl halides and tosylates in 60percent Me2SO/wares at 40 deg C, based on direct measurements of Bronsted β values for general base catalysis by oxyanion buffers, Hammet ρ values, and β1g for substituted quinuclidines.The Bronsted slopes increase from β - 0.67 for N-(2-(p-nitrophenyl)ethyl)quinuclidinium ions, which react by an E1cBirr mechanism, to β ca. 0.9 for the reactions of other N-(2-arylethyl)quinuclidinium ions by a concerted E2 elimination.There is no detectable interaction between the base catalyst and the leaving group for E1cB elimination, so that the interaction coefficient pxy = dβ1g/dpKBH = dβ/dpK1g is ca.0 for the N-(2-(p-nitrophenyl)ethyl)quinuclidinium ions.In contrast, values of β1g become less negative with increasing pKa of the base catalyst for the p-cyano and other N-(2-arylethyl)quinuclidinium ions, giving a constant value of pxy = 0.018 for the E2 elimination reactions of these compounds.The positive pxy coefficient for the N-(2-phenylethyl)quinuclidinium ions is confirmed by the observation of less negative values of β1g as the effective basicity of aqueous tetramethylammonium hydroxyde is increased by the addition of Me2SO.An increase in β with poorer leaving groups in the series of 2-(p-nitrophenyl)ethyl halides also corresponds to a positive pxy coefficient and an E2 mechanism.The interaction between the leaving group and central atoms is shown by the less negative values of β1g with electron-withdrawing substituents on the β-phenyl group, which corresponds to a negative coefficient pyy' = -dβ1g/d?- = -dρ/dpK1g = -0.09.A small decrease in β with electron-withdrawing substituents on the β-phenyl group suggests an interaction between the base catalyst and the central atoms that is described by a negative coefficient pxy' = dβ/d?- = dρ/dpKBH = -0.07.The sign of the pyy' and pxy' coefficient are consistent with an important component of proton transfer in the transition state.These properties of the E2 elimination reactions of N-(2-arylethyl)quinuclidinium ions can be described by a reaction coordinate that is rotated 24 deg counterclockwise from the x coordinate (for proton transfer) on a reaction coordinate-energy diagram that is defined by the observed structure-reactivity parameters.In contrast, β increases with increasing ? for elimination reactions of 2-arylethyl bromides with a positive value of pxy' = 0.07.This suggests more diagonal character to the transition state on the reaction coordinate diagram.The change from E1cB to an E2 mechanism is more easily described as a transformation of mechanism than as a change between two coexisting mechanisms.