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
ANTIBACTERIAL COMPOUNDS
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Page/Page column 26, (2012/04/18)
The present invention provides a compound of the following formula and salts thereof: Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
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.
