99860-38-5

Upstream product

• 4838-56-6 N-(4-methoxyphenyl)imidodicarbonimidic diamide hydrochloride 
• 96-34-4 methyl chloroacetate 
• 104-94-9 4-methoxy-aniline 
• 105-39-5 chloroacetic acid ethyl ester 

Downstream Products

• 1269527-25-4 6-{[4-(benzylideneamino)-5-phenyl-4H-1,2,4-triazol-3-ylthio]methyl}-N₂-(4-methoxyphenyl)-1,3,5-triazine-2,4-diamine 
• 1269527-15-2 6-[(1H-benzo[d]imidazol-2-ylthio)methyl]-N₂-(4-methoxyphenyl)-1,3,5-triazine-2,4-diamine 
• 1269527-27-6 6-{[4-(4-bromobenzylideneamino)-5-phenyl-4H-1,2,4-triazol-3-ylthio]methyl}-N₂-(4-methoxyphenyl)-1,3,5-triazine-2,4-diamine 
• 1269527-21-0 6-[(4,5-diphenyl-4H-1,2,4-triazol-3-ylthio)methyl]-N₂-(4-methoxyphenyl)-1,3,5-triazine-2,4-diamine 
• 1269527-23-2 N₂-(4-methoxyphenyl)-6-{[4-phenyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-ylthio]methyl}-1,3,5-triazine-2,4-diamine 
• 1269527-20-9 N₂-(4-methoxyphenyl)-6-((5-methyl-1H-benzo[d]imidazol-2-ylthio)methyl)-1,3,5-triazine-2,4-diamine 

Relevant academic research and scientific papers

Identifying Lysophosphatidic Acid Acyltransferase β (LPAAT-β) as the Target of a Nanomolar Angiogenesis Inhibitor from a Phenotypic Screen Using the Polypharmacology Browser PPB2

By screening a focused library of kinase inhibitor analogues in a phenotypic co-culture assay for angiogenesis inhibition, we identified an aminotriazine that acts as a cytostatic nanomolar inhibitor. However, this aminotriazine was found to be completely inactive in a whole-kinome profiling assay. To decipher its mechanism of action, we used the online target prediction tool PPB2 (http://ppb2.gdb.tools), which suggested lysophosphatidic acid acyltransferase β (LPAAT-β) as a possible target for this aminotriazine as well as several analogues identified by structure–activity relationship profiling. LPAAT-β inhibition (IC50 ≈15 nm) was confirmed in a biochemical assay and by its effects on cell proliferation in comparison with a known LPAAT-β inhibitor. These experiments illustrate the value of target-prediction tools to guide target identification for phenotypic screening hits and significantly expand the rather limited pharmacology of LPAAT-β inhibitors.

Synthesis and antiviral activity of benzimidazolyl-and triazolyl-1,3,5- triazines

A novel series of 1,3,5-triazine analogs was successfully synthesized through conjugation with benzimidazole or 1,2,4-triazole derivatives via a methylenethio linker. The new analogs were in vitro evaluated against HSV-1 in Vero cells; among these analogs, two compounds exhibited good effect in inhibiting HSV-1 replication (for compound 5p: EC50 = 3.5 μg/ml, SI = 358; for compound 5r: EC50 = 5.0 μg/ml, SI = 300) in comparison to acyclovir. Springer Science+Business Media, LLC 2011.