906480-89-5

Upstream product

• 932033-70-0 3-dimethylamino-2-(4-methoxy-phenyl)-1-(3,4,5-trimethoxy-phenyl)-propenone 
• 932033-68-6 2-(4-methoxy-benzyl)-2-(3,4,5-trimethoxy-phenyl)-[1,3]dithiane 
• 57009-70-8 2-(3,4,5-trimethoxyphenyl)-1,3-dithiane 
• 86-81-7 3,4,5-trimethoxy-benzaldehyde 
• 205366-78-5 2-(4-methoxyphenyl)-1-(3,4,5-trimethoxyphenyl)ethane-1-one 
• 851729-15-2 [3-(4-methoxy-phenyl)-oxiranyl]-(3,4,5-trimethoxy-phenyl)-methanone 
• 105-13-5 4-Methoxybenzyl alcohol 
• 118-41-2 Eudesmic acid 
• 824-94-2 p-methoxybenzyl chloride 
• 4521-61-3 3,4,5-Trimethoxybenzoyl chloride 
• 123-11-5 4-methoxy-benzaldehyde 

Relevant academic research and scientific papers

Sea Urchin Embryo Model As a Reliable in Vivo Phenotypic Screen to Characterize Selective Antimitotic Molecules. Comparative evaluation of Combretapyrazoles, -isoxazoles, -1,2,3-triazoles, and -pyrroles as Tubulin-Binding Agents

A series of both novel and reported combretastatin analogues, including diarylpyrazoles, -isoxazoles, -1,2,3-triazoles, and -pyrroles, were synthesized via improved protocols to evaluate their antimitotic antitubulin activity using in vivo sea urchin embryo assay and a panel of human cancer cells. A systematic comparative structure-activity relationship studies of these compounds were conducted. Pyrazoles 1i and 1p, isoxazole 3a, and triazole 7b were found to be the most potent antimitotics across all tested compounds causing cleavage alteration of the sea urchin embryo at 1, 0.25, 1, and 0.5 nM, respectively. These agents exhibited comparable cytotoxicity against human cancer cells. Structure-activity relationship studies revealed that compounds substituted with 3,4,5-trimethoxyphenyl ring A and 4-methoxyphenyl ring B displayed the highest activity. 3-Hydroxy group in the ring B was essential for the antiproliferative activity in the diarylisoxazole series, whereas it was not required for potency of diarylpyrazoles. Isoxazoles 3 with 3,4,5-trimethoxy-substituted ring A and 3-hydroxy-4-methoxy-substituted ring B were more active than the respective pyrazoles 1. Of the azoles substituted with the same set of other aryl pharmacophores, diarylpyrazoles 1, 4,5-diarylisoxazoles 3, and 4,5-diaryl-1,2,3-triazoles 7 displayed similar strongest antimitotic antitubulin effect followed by 3,4-diarylisoxazoles 5, 1,5-diaryl-1,2,3-triazoles 8, and pyrroles 10 that showed the lowest activity. Introduction of the amino group into the heterocyclic core decreased the antimitotic antitubulin effect of pyrazoles, triazoles, and to a lesser degree of 4,5-diarylisoxazoles, whereas potency of the respective 3,4-diarylisoxazoles was increased.

COMPOUNDS FOR THE TREATMENT OF ANGIOGENESIS

The invention relates to isoxazole, isothiazole, and triazole compounds that are useful for treating or inhibiting angiogenesis.

Synthesis and cytotoxic activities of 4,5-diarylisoxazoles

A series of 4,5-diarylisoxazoles related to combretastatin A-4 (CA-4) were synthesized and evaluated for cytotoxicity against three human cancer cell lines. Among them, compound 6e showed better cytotoxic activity than CA-4 in HeLa and HepG2 cell lines as

THIAZOLES FOR THE TREATMENT OF PROLIFERATIVE DISORDERS

The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polym

COMPOUNDS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS

The invention relates to compounds of structural formula (I); or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polym