94201-97-5Relevant academic research and scientific papers
Synthesis and biological evaluations of 1,2-diaryl pyrroles as analogues of combretastatin A-4
Sun, Jun,Chen, Lei,Liu, Chunjiang,Wang, Zhan,Zuo, Daiying,Pan, Jiatong,Qi, Huan,Bao, Kai,Wu, Yingliang,Zhang, Weige
, p. 1541 - 1547 (2016/02/05)
A series of novel 1,2-diaryl pyrroles as analogues of combretastatin A-4 (CA-4, 1a) were synthesized and evaluated for their antitumour potential against three cancer cell lines. Most compounds exhibited growth inhibition against all of the cancer cell lines. Compound 7q not only exhibited prominent antitumour efficacy with IC50 values of 0.390 μm in SGC-7901, 0.070 μm in HT-1080 and 0.045 μm in KB cell lines but also showed low activity with IC50 values of 30.08 μm in normal L929 cell line. Moreover, compound 7q inhibited tubulin polymerization into microtubules and caused microtubule destabilization. A molecular docking study of 7q was performed to determine its binding mode at the colchicine site in the tubulin dimer. 1,2-Diaryl pyrroles as combretastatin A-4 analogues were synthesized and evaluated for anti-proliferative activities. Compound 7q exhibited antitubulin activity.
Efficient synthesis of uracil-derived hexa- and tetrahydropyrido[2,3-d] pyrimidines
Tolstoluzhsky, Nikita,Nikolaienko, Pavlo,Gorobets, Nikolay,Van Der Eycken, Erik V.,Kolos, Nadezhda
supporting information, p. 5364 - 5369 (2013/09/02)
A reaction of 6-amino-1,3-dimethyluracil with 3-(hetero)aroylacrylic acids and their methyl esters leads to hexahydropyrido[2,3-d]pyrimidine-5-carboxylic acids or the corresponding methyl esters in high to excellent yields. One-pot oxidation of the acid d
Arylalkane, arylalkene and aryl azaalkane, medicaments containing said compounds and method for the production thereof
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Page/Page column 63-64, (2010/11/27)
The present invention relates to compounds of general formula [in-line-formulae]R—Z1—Z2—Z3—R1, ??(I)[/in-line-formulae] wherein R, R1 and Z1 to Z3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
A New Method for the Preparation of (E)-3-Acylprop-2-enoic Acids
Obrecht, Daniel,Weiss, Bettina
, p. 117 - 122 (2007/10/02)
A new method for the preparation of (E)-3-acylprop-2-enoic acids ( = (E)-3-acylacrylic acids) of type II via acid catalyzed isomerization of the corresponding 3-acylprop-2-ynal acetals of type I (Scheme 1) has been found.The described reaction gives a rap
Gastric anti-secretory, anti-ulcer and cytoprotective properties of substituted (E)-4-phenyl- and heteroaryl-4-oxo-2-butenoic acids
Bianchi, Mario,Butti, Alina,Christidis, Yani,Perronnet, Jacques,Barzaghi, Fernando,et al.
, p. 45 - 52 (2007/10/02)
A class of anti-secretory, anti-ulcer and cytoprotective agents, the substituted (E)-4-phenyl and heteroaryl-4-oxo-2-butenoic acids, is described.This chemical structure is not related to those of any known anti-cholinergic drugs, histamine H2-receptor antagonists or prostaglandins.Five compounds, 4-(2-methoxyphenyl)- 15, 4-(4-methoxyphenyl)- 22, 4-(3,4-dimethoxyphenyl)- 32, 4-(3,4,5-trimethoxyphenyl)- 40, and 4-(2-furanyl)-4-oxo-2-butenoic acid 44, have cytoprotective activity at a very low dose (0.6 mg/kg, p.o.) and anti-secretory and anti-ulcer activities at higher doses.One of these compounds, RU 38086 40, has been selected for clinical evaluation.Keywords - anti-ulcer agents / cytoprotective agents / (E)-4-phenyl- and heteroaryl-4-oxo-2-butenoic acids.
Derivatives of phenyl aliphatic carboxylic acids, and use thereof in treating gastric and gastro-duodenal ailments
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, (2008/06/13)
A compound of the formula (I) STR1 in which the three methoxy radicals are in the 3,4,5, or 2,4,6 or 2,4,5 or 2,3,5 or 2,3,6 positions, in which either A and B together represent a double bond or else A represents a hydrogen atom and B represents a hydrox
