945762-01-6

Upstream product

• 106261-48-7 4-(4-methylpiperazin-1-ylmethyl)benzoic acid 
• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 
• 148077-69-4 4-(4-Methylpiperazin-1-ylmethyl)benzoyl chloride 
• 1117-97-1 N,0-dimethylhydroxylamine 

Downstream Products

• 933986-40-4 1-(4-ethynylbenzyl)-4-methylpiperazine 
• 439691-80-2 4-((4-methylpiperazin-1-yl)methyl)benzaldehyde 
• 1346617-86-4 N-[2-methyl-5-(4-{4-[(4-methylpiperazin-1-yl)methyl]phenyl}-1H-1,2,3-triazol-1-yl)phenyl]-4-(pyridine-3-yl)pyrimidin-2-amine 

Relevant academic research and scientific papers

Heterocycle compound containing triazole, as well as preparation method and application of heterocycle compound

The invention provides a heterocycle compound containing triazole, as well as a preparation method and application of the heterocycle compound. The heterocycle compound containing the triazole has a general formula in the following structure (as shown in

Syntheses and biological evaluation of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib

Three novel series of 1,2,3-triazole and 1,3,4-oxadiazole derivatives of imatinib were prepared and evaluated in vitro for their cytostatic effects against a human chronic myeloid leukemia (K562), acute myeloid leukemia (HL60), and human leukemia stem-like cell line (KG1a). The structure-activity relationship was analyzed by determining the inhibitory rate of each imatinib analog. Benzene and piperazine rings were necessary groups in these compounds for maintaining inhibitory activities against the K562 and HL60 cell lines. Introducing a trifluoromethyl group significantly enhanced the potency of the compounds against these two cell lines. Surprisingly, some compounds showed significant inhibitory activities against KG1a cells without inhibiting common leukemia cell lines (K562 and HL60). These findings suggest that these compounds are able to inhibit leukemia stem-like cells.

Identification of a series of highly potent activators of the Nurr1 signaling pathway

The nuclear receptor Nurr1 (NR4A2) is critically involved in the development and maintenance of midbrain dopaminergic neurons and is believed to function independently of endogenous activation. The hit identification and SAR studies leading to isoxazolo-pyridinone 7e, a highly potent, brain penetrable activator of the Nurr1 signaling pathway, are described.