Category: 287114-25-4

Hendrick, Charles E.; Jorgensen, Jeff R.; Chaudhry, Charu; Strambeanu, Iulia I.; Brazeau, Jean-Francois; Schiffer, Jamie; Shi, Zhicai; Venable, Jennifer D.; Wolkenberg, Scott E. published the artcile< Direct-to-Biology Accelerates PROTAC Synthesis and the Evaluation of Linker Effects on Permeability and Degradation>, Reference of 287114-25-4, the main research area is proteolysis targeting chimera preparation linker effect.

A platform to accelerate optimization of proteolysis targeting chimeras (PROTACs) had been developed using a direct-to-biol. (D2B) approach with a focus on linker effects. A large number of linker analogs-varying length, polarity, and rigidity-were rapidly prepared and characterized in four cell-based assays by streamlining time-consuming steps in synthesis and purification The expansive data set informs on linker structure activity relationships for in-cell E3 ligase target engagement, degradation, permeability, and cell toxicity. Unexpected aspects of linker SAR were discovered, consistent with literature reports on “”linkerol.””, and the method dramatically speeds up empirical optimization. Physicochem. property trends emerged, and the platform had the potential to rapidly expand training sets for more complex prediction models. In-depth validation studies were carried out and confirm the D2B platform was a valuable tool to accelerate PROTAC design-make-test cycles.

ACS Medicinal Chemistry Letters published new progress about Chemical library. 287114-25-4 belongs to class esters-buliding-blocks, and the molecular formula is C12H22N2O2, Reference of 287114-25-4.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Park, Eunsun; Lee, Sun Joo; Moon, Heegyum; Park, Jongmi; Jeon, Hyeonho; Hwang, Ji Sun; Hwang, Hayoung; Hong, Ki Bum; Han, Seung-Hee; Choi, Sun; Kang, Soosung published the artcile< Discovery and Biological Evaluation of N-Methyl-pyrrolo[2,3-b]pyridine-5-carboxamide Derivatives as JAK1-Selective Inhibitors>, Electric Literature of 287114-25-4, the main research area is methyl pyrrolopyridine carboxamide preparation Janus kinase inhibitor mol docking.

Janus kinase 1 (JAK1) plays a key role in most cytokine-mediated inflammatory and autoimmune responses through JAK/STAT signaling; thus, JAK1 inhibition is a promising therapeutic strategy for several diseases. Anal. of the binding modes of current JAK inhibitors to JAK isoforms allowed the design of N-alkyl-substituted 1-H-pyrrolo[2,3-b] pyridine carboxamides I (R = H, Me, cyclopropyl, cyclopentyl) as a JAK1-selective scaffold, and the synthesis of various Me amide derivatives e.g., II, provided III as a potent JAK1-selective inhibitor. In particular, the (S,S)-enantiomer of III exhibited excellent potency for JAK1 and selectivity over JAK2, JAK3, and TYK2. On investigating the effect of III on hepatic fibrosis, it was found that it reduces the proliferation and fibrogenic gene expression of TGF-灏?induced hepatic stellate cells (HSCs). Specifically, III significantly inhibited TGF-灏?induced migration of HSCs at 0.25娓璏 in wound-healing assays.

Journal of Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 287114-25-4 belongs to class esters-buliding-blocks, and the molecular formula is C12H22N2O2, Electric Literature of 287114-25-4.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Park, Eunsun; Lee, Sun Joo; Moon, Heegyum; Park, Jongmi; Jeon, Hyeonho; Hwang, Ji Sun; Hwang, Hayoung; Hong, Ki Bum; Han, Seung-Hee; Choi, Sun; Kang, Soosung published the artcile< Discovery and Biological Evaluation of N-Methyl-pyrrolo[2,3-b]pyridine-5-carboxamide Derivatives as JAK1-Selective Inhibitors>, Electric Literature of 287114-25-4, the main research area is methyl pyrrolopyridine carboxamide preparation Janus kinase inhibitor mol docking.

Janus kinase 1 (JAK1) plays a key role in most cytokine-mediated inflammatory and autoimmune responses through JAK/STAT signaling; thus, JAK1 inhibition is a promising therapeutic strategy for several diseases. Anal. of the binding modes of current JAK inhibitors to JAK isoforms allowed the design of N-alkyl-substituted 1-H-pyrrolo[2,3-b] pyridine carboxamides I (R = H, Me, cyclopropyl, cyclopentyl) as a JAK1-selective scaffold, and the synthesis of various Me amide derivatives e.g., II, provided III as a potent JAK1-selective inhibitor. In particular, the (S,S)-enantiomer of III exhibited excellent potency for JAK1 and selectivity over JAK2, JAK3, and TYK2. On investigating the effect of III on hepatic fibrosis, it was found that it reduces the proliferation and fibrogenic gene expression of TGF-�induced hepatic stellate cells (HSCs). Specifically, III significantly inhibited TGF-�induced migration of HSCs at 0.25渭M in wound-healing assays.

Journal of Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 287114-25-4 belongs to class esters-buliding-blocks, and the molecular formula is C12H22N2O2, Electric Literature of 287114-25-4.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Canale, Vittorio; Frisi, Valeria; Bantreil, Xavier; Lamaty, Frederic; Zajdel, Pawel published the artcile< Sustainable Synthesis of a Potent and Selective 5-HT7 Receptor Antagonist Using a Mechanochemical Approach>, Quality Control of 287114-25-4, the main research area is benzenesulfonamide PZ1361 synthesis antidepressant serotonin 5HT7 receptor.

A mechanochem. procedure was developed to obtain PZ-1361, a potent and selective 5-HT7 receptor antagonist, with antidepressant properties in rodents. The elaborated protocol offered several advantages over classical batch synthesis, including improvement of the overall yield (from 34% to 64%), reduction of reaction time (from 60 to 5.5 h), limitation of the use of toxic solvents, and the formation of byproducts. This approach represents a rare example of the synthesis of biol. active compounds exclusively performed using mechanochem. reactions.

Journal of Organic Chemistry published new progress about 5-HT7 receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 287114-25-4 belongs to class esters-buliding-blocks, and the molecular formula is C12H22N2O2, Quality Control of 287114-25-4.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics