41727-70-2Relevant academic research and scientific papers
Application of quinoline derivatives of N-isostere tectorigenin in anti-hepatocarcinoma drugs
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Paragraph 0061-0063; 0069; 0072; 0079, (2018/11/03)
The invention discloses application of quinoline derivatives of N-isostere tectorigenin in anti-hepatocarcinoma drugs. The invention relates to the quinoline derivatives of the N-isostere tectorigenin, and the chemical structural formula of the quinoline
Synthesis method of quinoline derivatives
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Paragraph 0017; 0029-0032; 0039; 0047; 0054, (2017/12/29)
The invention discloses a synthesis method of quinoline derivatives. The method comprises steps shown in the description. According to the synthesis method of the quinoline derivatives, yield is high, the method is safe, environment-friendly, energy-savin
Synthetic method of 3-(4-methoxyphenyl)-6-methoxyl-4-chlorine-5, 7-dibromoquinoline
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Paragraph 0054; 0057, (2017/12/28)
The invention discloses a synthetic method of 3-(4-methoxyphenyl)-6-methoxyl-4-chlorine-5, 7-dibromoquinoline. The synthetic method includes the following steps. The synthetic method has the advantages that the yield is high, safety, environment protectio
Synthesis method of quinoline derivative
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Paragraph 0029; 0030; 0037; 0045; 0052, (2018/03/24)
The invention discloses a synthesis method of a quinoline derivative. The synthesis method includes the following steps in the specification. The method has high yield, is safe and environment-friendly, saves energy and reduces emission. The method is 90.
Synthesis method of quinoline derivative
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Paragraph 0029; 0030; 0031; 0032; 0039; 0046; 0052, (2018/01/11)
The invention discloses a synthesis method of a quinoline derivative. The synthesis method includes the following steps in the specification. The method has high yield, is safe and environment-friendly, saves energy and reduces emission. The method is 90.
Synthesizing method of 3-(4-methoxyphenyl)-6-methyoxyl-4-chloro-5, 7-dibromoquinoline
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Paragraph 0030; 0032; 0048; 0055, (2018/04/01)
The invention discloses a synthesizing method of a 3-(4-methoxyphenyl)-6-methyoxyl-4-chloro-5, 7-dibromoquinoline. The synthesizing method of the 3-(4-methoxyphenyl)-6-methyoxyl-4-chloro-5, 7-dibromoquinoline comprises the following steps of A. The synthe
Synthesis method of 3-(4-methoxyphenyl)-6-methoxy-4-chloro-5,7-dibromoquinoline
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Paragraph 0028; 0030; 0038; 0046; 0053, (2018/04/01)
The invention discloses a synthesis method of 3-(4-methoxyphenyl)-6-methoxy-4-chloro-5,7-dibromoquinoline. The synthesis method comprises the following steps: the steps are shown in the description. The synthesis method disclosed by the invention has the
Increased endothelial cell selectivity of triazole-bridged dihalogenated A-ring analogues of combretastatin A-1
Beale, Thomas M.,Bond, Peter J.,Brenton, James D.,Charnock-Jones, D. Stephen,Ley, Steven V.,Myers, Rebecca M.
scheme or table, p. 1749 - 1759 (2012/04/10)
The antiproliferative activity on ovarian cancer (SK-OV-3) cells of a series of triazole-bridged combretastatin analogues (37, 38, 40-43) containing dihalogenation of the A-ring is reported, and compared with their trimethoxy analogues (5, 15, 39). It was found that dihalogenation with either bromine or iodine was a tolerated modification when compared to the parent compound combretastatin (CA-4, 1) and had less effect than B-ring modification on potency. These compounds exhibited G2/M arrest, and maintained antitubulin activity. Further assays on human umbilical vein endothelial cells (HUVECs) demonstrated the potential antivascular effects of these triazoles. Of particular note was a 3,5-diiodo-4-methoxyaryl triazole (43) which had promising 7-fold selectivity for HUVECs over ovarian cancer cells.
A-ring dihalogenation increases the cellular activity of combretastatin-templated tetrazoles
Beale, Thomas M.,Allwood, Daniel M.,Bender, Andreas,Bond, Peter J.,Brenton, James D.,Charnock-Jones, D. Stephen,Ley, Steven V.,Myers, Rebecca M.,Shearman, James W.,Temple, Jill,Unger, Jessica,Watts, Ciorsdaidh A.,Xian, Jian
supporting information; experimental part, p. 177 - 181 (2012/05/05)
The combretastatins have been investigated for their antimitotic and antivascular properties, and it is widely postulated that a 3,4,5-trimethoxyaryl A-ring is essential to maintain potent activity. We have synthesized new tetrazole analogues (32a€"34), demonstrating that 3,5-dihalogenation can consistently increase potency by up to 5-fold when compared to the equivalent trimethoxy compound on human umbilical vein endothelial cells (HUVECs) and a range of cancer cells. Moreover, this increased potency offsets that lost by installing the tetrazole bridge into combretastatin A-4 (1), giving crystalline, soluble compounds that have low nanomolar activity, arrest cells in G2/M phase, and retain microtubule inhibitory activity. Molecular modeling has shown that optimized packing within the binding site resulting in increased Coulombic interaction may be responsible for this improved activity.
Products of reaction between tetrabromo-substituted ortho- and para-hydroxybenzoic acids and sodium nitrite in CH3COOH
Fadin,Tarasova,Vasin,Shishkin
, p. 1062 - 1070 (2013/01/15)
The reaction of 2,3,5,6-tetrabromo-4-hydroxybenzoic acid with a 10-fold excess of NaNO2 in the glacial acetic acid at 20°C affords tetrabromonitrosophenols whose further transformations under the reaction conditions leads to the formation of a mixture of 2,4,5,6-tetrabromo-p-quinone diazide and tetrabromo-p- and -o-nitrophenols in the molar ratio 37 : 2 : 1. Under similar conditions the 3,4,5,6-tetrabromo-2-hydroxybenzoic acid is converted into a mixture of 3,4,5,6-tetrabromo-o-quinone diazide with the same nitrophenols in the ratio 13 : 1 : 3. The reaction of sodium 2,3,5,6-tetrabromo-4-hydroxy-benzoate with NaNO2 in dilute acetic acid resulted in a quantitative yield of tetrabromo-p-quinone monooxime. Pleiades Publishing, Ltd., 2012.
