100388-41-8

Upstream product

• 3240-94-6 N-(2-chlorethyl)morpholine 
• 619-08-9 2-chloro-4-nitrophenol 
• 3647-69-6 4-(2-chloroethyl)morpholine hydrochride 
• 350-30-1 3-chloro-4-fluoronitrobenzene 
• 110-91-8 morpholine 

Downstream Products

• 100248-82-6 [3-chloro-4-(2-morpholin-4-ylethoxy)phenyl]amine 
• 1338251-29-8 1-[4'-(trifluoromethyl)phenyl]-4-[N-[3-chloro-4-(2'-morpholinoethoxy)phenyl]aminomethyl]-1H-1,2,3-triazole 
• 1338251-30-1 1-(2'-nitrophenyl)-4-[N-[3-chloro-4-(2'-morpholinoethoxy)phenyl]aminomethyl]-1H-1,2,3-triazole 
• 1338251-33-4 1-(2',4',6'-trichlorophenyl)-4-[N-[3-chloro-4-(2'-morpholinoethoxy)phenyl]aminomethyl]-1H-1,2,3-triazole 
• 1338251-34-5 1-(2'-chloro-4'-nitrophenyl)-4-[N-[3-chloro-4-(2'-morpholinoethoxy)phenyl]aminomethyl]-1H-1,2,3-triazole 
• 111271-83-1 [3-chloro-4-(2-morpholino-ethoxy)-phenyl]-carbamic acid ethyl ester; hydrochloride 

Relevant academic research and scientific papers

Synthesis and biological evaluation of morpholine-substituted diphenylpyrimidine derivatives (Mor-DPPYs) as potent EGFR T790M inhibitors with improved activity toward the gefitinib-resistant non-small cell lung cancers (NSCLC)

Potential new EGFRT790M inhibitors comprised of structurally modified diphenylpyrimidine derivatives bearing a morpholine functionality (Mor-DPPYs) were used to improve the activity and selectivity of gefitinib-resistant non-small cell lung cancer (NSCLC) treatment. This led to the identification of inhibitor 10c, which displayed high activity against EGFRT790M/L858R kinase (IC50?=?0.71?nM) and repressed H1975?cell replication harboring EGFRT790M mutations at a concentration of 0.037?μM. Inhibitor 10c demonstrated high selectivity (SI?=?631.9) for T790M-containing EGFR mutants over wild type EGFR, suggesting that it will cause less side effects. Moreover, this compound also shows promising antitumor efficacy in a murine EGFRT790M/L858R-driven H1975 xenograft model without affecting body weight. This study provides new potential lead compounds for further development of anti-NSCLC drugs.

Discovery of biphenyl-based VEGFR-2 inhibitors. Part 3: Design, synthesis and 3D-QSAR studies

VEGFR-2 plays an essential role in angiogenesis and is a central target for anticancer drug discovery. In order to develop novel VEGFR-2 inhibitors, we designed and synthesized 33 biphenyl amides based on our previously reported lead compound. The biological results indicated that four compounds (18b, 20e, 20h and 20j) are potent VEGFR-2 inhibitors which are comparable to positive control. Compound 18b displayed the most potent VEGFR-2 inhibition with IC50 value of 2.02 nM. Moreover, it exhibited promising antiproliferative activity against MCF-7 and SMMC-7721 cells with IC50 values of 1.47 μM and 5.98 μM, respectively. Molecular docking and 3D-QSAR studies were also carried out. The results indicated that these biphenyl amides could serve as promising leads for further optimization as novel VEGFR-2 inhibitors.

Synthesis and Biological Activity of Novel 1-Substituted Phenyl-4-[N-[(2'-morpholinothoxy)phenyl]aminomethyl]-1H-1,2,3-Triazoles

In an attempt to search for potent antifungal agents, a series of novel 1-substituted phenyl-4-[N-[(2'-morpholinothoxy)phenyl]aminomethyl]-1H-1,2,3-triazoles 5a-m was designed and synthesized via Huisgen cycloaddition reaction between various (2-morpholin