1421372-76-0Relevant articles and documents
Refinement of covalent EGFR inhibitor AZD9291 to eliminate off-target activity
Bouffard, Elise,Cravatt, Benjamin,Dix, Melissa M.,Wong, Chi-Huey,Zaro, Balyn W.
, (2021/05/29)
Non-small-cell lung cancer (NSCLC) is a major disease that accounts for 85% of all lung cancer cases which claimed around 1.8 billion lives worldwide in 2020. Tyrosine kinase inhibitors (TKIs) that target EGFR have been used for the treatment of NSCLC, but often develop drug resistance, and the covalent inhibitor AZD9291 has been developed to tackle the problem of drug resistance mediated by the T790M EGFR mutation; however, there is a side effect of hyperglycemia that may be due to off-target activity. This study examines analogs of AZD9291 by chemical proteomics, identifying analogs that maintain T790M-EGFR engagement while showing reduced cross-reactivity with off-targets.
P-phenylenediamine LSD1 inhibitor and preparation method thereof
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Paragraph 0112; 0119-0122, (2021/09/08)
Disclosed are a p-phenylenediamine derivative as represented by general formula I, a pharmaceutically acceptable salt, and a stereoisomer thereof. The p-phenylenediamine derivative as represented by general formula I, the pharmaceutically acceptable salt thereof and the stereoisomer thereof can be used alone or in combination as lysine-specific demethylase-1 (LSD1) inhibitors.
4-indole-2-arylaminopyrimidine compound and application thereof in inflammation treatment
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, (2020/05/05)
The invention belongs to the field of medicinal chemistry, and particularly discloses an N-(4-(1-methyl-1H-indole-3-yl) pyrimidine-2-yl)benzene-1,3-diamine analogue shown as the following formula (I),in the formula, R1 is selected from H, halogen or C1-C5 alkoxy, R2 is selected from H, halogen a C1-C12 chain alkyl substituted nitrogen-containing group, a C3-C6 cyclic group substituted nitrogen-containing group, a five-membered nitrogen-containing heterocyclic ring, a six-membered nitrogen-containing heterocyclic ring or a seven-membered nitrogen-containing heterocyclic ring. The invention further discloses an application of the compound shown in the formula (I) in preparation of drugs for inflammation-related diseases, and pharmacological results show that the N-(4-(1-methyl-1H-indol-3-yl)pyrimidine-2-yl)benzene-1,3-diamine analogue can effectively inhibit release of IL-6 and IL-8 inflammatory factors and has good anti-inflammatory activity.