77377-04-9

Upstream product

• 100-43-6 4-vinylpyridine 
• 95-56-7 2-hydroxybromobenzene 
• 108-89-4 picoline 
• 90-02-8 salicylaldehyde 

Downstream Products

• 872811-66-0 2-(2-[4]pyridyl-ethyl)-phenol 
• 132951-79-2 1-(4-Bromo-butyl)-4-[(E)-2-(2-hydroxy-phenyl)-vinyl]-pyridinium; bromide 
• 79131-25-2 1-Butoxycarbonylmethyl-4-[(E)-2-(2-hydroxy-phenyl)-vinyl]-pyridinium; chloride 
• 132951-80-5 1-(5-Bromo-pentyl)-4-[(E)-2-(2-hydroxy-phenyl)-vinyl]-pyridinium; bromide 
• 132951-81-6 1-(6-Bromo-hexyl)-4-[(E)-2-(2-hydroxy-phenyl)-vinyl]-pyridinium; bromide 
• 79131-30-9 4-[(E)-2-(2-Hydroxy-phenyl)-vinyl]-1-(1-methoxycarbonyl-ethyl)-pyridinium; bromide 
• 79131-32-1 4-[(E)-2-(2-Hydroxy-phenyl)-vinyl]-1-(1-propoxycarbonyl-ethyl)-pyridinium; bromide 
• 79131-33-2 1-(1-Butoxycarbonyl-ethyl)-4-[(E)-2-(2-hydroxy-phenyl)-vinyl]-pyridinium; bromide 
• 79131-24-1 4-[(E)-2-(2-Hydroxy-phenyl)-vinyl]-1-propoxycarbonylmethyl-pyridinium; chloride 
• 79131-28-5 4-[(E)-2-(2-Hydroxy-phenyl)-vinyl]-1-propoxycarbonylmethyl-pyridinium; bromide 
• 79131-29-6 1-Butoxycarbonylmethyl-4-[(E)-2-(2-hydroxy-phenyl)-vinyl]-pyridinium; bromide 
• 139748-93-9 (E)-N-p-Nitrobenzyl-γ-azastilbenol-2' chloride 
• 139748-91-7 (E)-N-o-Nitrobenzyl-γ-azastilbenol-2' chloride 
• 79131-34-3 1-Benzyl-4-[(E)-2-(2-hydroxy-phenyl)-vinyl]-pyridinium; chloride 

Relevant academic research and scientific papers

Fluoroethoxy-1,4-diphenethylpiperidine and piperazine derivatives: Potent and selective inhibitors of [3H]dopamine uptake at the vesicular monoamine transporter-2

A small library of fluoroethoxy-1,4-diphenethyl piperidine and fluoroethoxy-1,4-diphenethyl piperazine derivatives were designed, synthesized and evaluated for their ability to inhibit [3H]dopamine (DA) uptake at the vesicular monoamine transporter-2 (VMAT2) and dopamine transporter (DAT), [3H]serotonin (5-HT) uptake at the serotonin transporter (SERT), and [3H]dofetilide binding at the human-ether-a-go-go-related gene (hERG) channel. The majority of the compounds exhibited potent inhibition of [3H]DA uptake at VMAT2, Ki changes in the nanomolar range (Ki = 0.014–0.073 μM). Compound 15d exhibited the highest affinity (Ki = 0.014 μM) at VMAT2, and had 160-, 5-, and 60-fold greater selectivity for VMAT2 vs. DAT, SERT and hERG, respectively. Compound 15b exhibited the greatest selectivity (>60-fold) for VMAT2 relative to all the other targets evaluated, and 15b had high affinity for VMAT2 (Ki = 0.073 μM). Compound 15b was considered the lead compound from this analog series due to its high affinity and selectivity for VMAT2.

Anti-Angiogenic Compounds

Compounds and compositions are described which are useful especially for treatment of angiogenesis-related diseases or disorders such as neovascularisation of the eye, age-related macular degeneration, diabetic retinopathy or cancer.

Inhibitory effect of cytotoxic nitrogen-containing heterocyclic stilbene analogues on VEGF protein secretion and VEGF, hTERT and c-Myc gene expression

A group of 21 nitrogen-containing heterocyclic stilbene derivatives, prepared by means of Heck coupling reactions, has been investigated for their cytotoxicity as well as their ability to inhibit the production of the vascular endothelial growth factor (VEGF) and the activation of telomerase. The ability of these compounds to inhibit proliferation of two tumoral cell lines (HT-29 and MCF-7) and one non-tumoral cell line (HEK-293) was first determined. Subsequently, we determined the capacity of the compounds to inhibit the secretion of VEGF in the aforementioned cell lines and downregulate the expression of the VEGF, hTERT and c-Myc genes, of which the latter two are involved in controlling the activation of telomerase.

ANTI-ANGIOGENIC COMPOUNDS

Compounds of the formula A-X-Y-B and compositions are described which are useful especially for treatment of angiogenesis-related diseases or disorders such as neovascularisation of the eye, age- related macular degeneration, diabetic retinopathy or cancer, wherein A is a six membered heteroaryl ring containing 2 nitrogen atoms which is optionally substituted with R1; R1 is H, CI-6 alkyl, CN, CONR2R3; R2 and R3 which may be the same or different and selected from H, CI-6 alkyl or R2 and R3 form a ring; the group X-Y is an alkyne or alkene, in the case wherein X-Y is an alkene the double bond may be cis or trans and optionally substituted with R1 B is an aryl; or five or six membered heteroaryl ring containing 1 to 3 heteroatoms, both of which may optionally substituted with one or more R4; R4 is R1 or OR5; R5 is H, COR6 or R6; and R6 is CI-6 alkyl and salts thereof.