78004-28-1

Upstream product

• 78004-26-9 N-<2-Hydroxy-2-(3-benzyloxy-4-methoxyphenyl)ethyl>formamide 
• 2426-87-1 3-methoxy-4-(phenylmethoxy)benzaldehyde 
• 22483-09-6 2,2-dimethoxyethylamine 
• 100-39-0 benzyl bromide 
• 621-59-0 isovanillin 
• 100-97-0 hexamethylenetetramine 
• 36455-21-7 3-benzyloxy-4-methoxyphenylethylamine 
• 1064206-87-6 6-benzyloxy-4-hydroxy-7-methoxy-1,2,3,4-tetrahydroisoquinoline 
• 1064206-95-6 2-tert-butoxycarbonyl-4-ethoxy-6-benzyloxy-7-methoxy-3,4-dihydro-1H-isoquinoline 
• 71146-40-2 5-(3-benzyloxy-4-methoxy-phenyl)-4,5-dihydro-oxazole 
• 63909-29-5 (E)-2-(benzyloxy)-1-methoxy-4-(2-nitrovinyl)benzene 
• 6346-05-0 3-benzyloxy-4-methoxybenzaldehyde 
• 1064206-90-1 2-tert-butoxycarbonyl-6-benzyloxy-7-methoxy-3,4-dihydro-1H-isoquinoline-4-ol 
• 1064206-86-5 N-(4-benzyloxy-3-methoxybenzyl)-N-(2,2-diethoxyethyl)amine 

Downstream Products

• 109849-38-9 N-formyl-6-benzyloxy-7-methoxy-1,2,3,4-tetrahydroisoquinoline 

Relevant academic research and scientific papers

Isoquinoline-based biaryls as a robust scaffold for microtubule inhibitors

We here report the discovery of isoquinoline-based biaryls as a new scaffold for colchicine domain tubulin inhibitors. Colchicinoid inhibitors offer highly desirable cytotoxic and vascular disrupting bioactivities, but their further development requires improving in vivo robustness and tolerability: properties that both depend on the scaffold structure employed. We have developed isoquinoline-based biaryls as a novel scaffold for high-potency tubulin inhibitors, with excellent robustness, druglikeness, and facile late-stage structural diversification, accessible through a tolerant synthetic route. We confirmed their bioactivity mechanism in vitro, developed soluble prodrugs, and established safe in vivo dosing in mice. By addressing several problems facing the current families of inhibitors, we expect that this new scaffold will find a range of in vivo applications towards translational use in cancer therapy.

ISOQUINOLINE BIARYL COMPOUNDS, A PHARMACEUTICAL COMPOSITION COMPRISING THE SAME, AND USES THEREOF

The present invention provides a compound having the formula (I) which is suitable as a tubulin polymerization inhibitor and/or an antimitotic cytotoxin. Thus, it can be employed in the treatment, amelioration or prevention of a disorder selected from a neoplastic disorder, atherosclerosis, psoriasis, restenosis, idiopathic pulmonary fibrosis, scleroderma, wet age-related macular degeneration, and cirrhosis of the liver.

The synthesis of precursor of FP- (+) DTBZ

A synthetic route to the precursor of FP- (+) DTBZ was disclosed, in which 3-hydroxy-4-methoxybenzaldehyde was employed as a starting material. In the method, the benzyl-protecting protocol and the in-situ Diels-Alder reaction made the procedure more practical because of the mild conditions for selectively deprotection and the accelerated reaction process.