Synthesis and Characterization of some Novel Quinoxaline-2, 3-Dione Derivatives: A Preliminary Investigation on their Activity Against a Human Epithelial Carcinoma Cell Line
About: This article is published in Letters in Drug Design & Discovery.The article was published on 2011-05-01. It has received 9 citations till now. The article focuses on the topics: Quinoxaline.
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TL;DR: Modifications of different fatty acids with existing anticancer drugs and heterocyclic moieties by condensation reactions increased the tissue selectivity and made chemotherapy potentially more effective and less toxic in in vivo and in vitro studies.
68 citations
30 Nov 2019
TL;DR: This examination gives proof to thought of profitable ligands in isoxazole substituted 9-anilinoacridines as potential HER2 inhibitor and the compounds, 1s,x,v,a,j,r with noteworthy Glide scores may deliver critical enemy of bosom malignant growth movement for further examinations may demonstrate their remedial potential.
Abstract: BACKGROUND Human Epidermal development factor Receptor-2 (HER2) is a membrane tyrosine kinase which is overexpressed and gene amplified in human breast cancers. HER2 amplification and overexpression have been linked to important tumor cell proliferation and survival pathways for 20% of instances of breast cancer. 9-aminoacridines are significant DNA-intercalating agents because of their antiproliferative properties. OBJECTIVE Some novel isoxazole substituted 9-anilinoacridines(1a-z) were designed by in-silico technique for their HER2 inhibitory activity. Docking investigations of compounds 1a-z are performed against HER2 (PDB id-3PP0) by using Schrodinger suit 2016-2. METHODS Molecular docking study for the designed molecules 1a-z are performed by Glide module, in-silico ADMET screening by QikProp module and binding free energy by Prime-MMGBSA module of Schrodinger suit. The binding affinity of designed molecules 1a-z towards HER2 was chosen based on GLIDE score. RESULTS Many compounds showed good hydrophobic communications and hydrogen bonding associations to hinder HER2. The compounds 1a-z, aside from 1z have significant Glide scores in the scope of - 4.91 to - 10.59 when compared with the standard Ethacridine (- 4.23) and Tamoxifen (- 3.78). The in-silico ADMET properties are inside the suggested about drug likeness. MM-GBSA binding of the most intense inhibitor is positive. CONCLUSION The outcomes reveal that this study provides evidence for the consideration of isoxazole substituted 9-aminoacridine derivatives as potential HER2 inhibitors. The compounds, 1s,x,v,a,j,r with significant Glide scores may produce significant anti breast cancer activity and further in vitro and in vivo investigations may prove their therapeutic potential.
24 citations
TL;DR: The results obtained in the biological assays against T. vaginalis indicate that compounds with ω-(dialkylamino)alkyl substituents and a keto group at positions 4 and 2 of quinoxaline ring provide interesting structural cores to develop novel prototypes to enhance the nitroquinoxalinones activity as trichomonacidal agents with interesting ADME properties according to virtual screening analysis.
14 citations
TL;DR: The Flash chromatography system plays a major role in improving the yield for the isolation of methyl gamma linolenate from Spirulina platensis and the isolated molecule is a potent cytotoxic agent towards human lung carcinoma cell lines, however it may be further taken up for an extensive study.
Abstract: Isolation of methyl gamma linolenate from Spirulina platensis using flash chromatography and its apoptosis inducing effect against human lung carcinoma A- 549 cell lines. Gamma linolenic acid is an important omega-6 polyunsaturated fatty acid (PUFA) of medicinal interest was isolated from microalgae Spirulina platensis using flash chromatography system (Isolera system) as its methyl ester. The isolated methyl gamma linolenate was characterized by IR, 1H NMR, 13C NMR and mass spectral analysis and the data were consistent with the structure. The percentage yield of isolated methyl gamma linolenate is found to be 71 % w/w, which is a very good yield in comparison to other conventional methods. It was subjected to in-vitro cytotoxic screening on A-549 lung cancer cell lines using SRB assay and result was compared with standard rutin. It may be concluded that the Flash chromatography system plays a major role in improving the yield for theisolation of methyl gamma linoleate from Spirulina platensis and the isolated molecule is a potent cytotoxicagent towards human lung carcinoma cell lines, however it may be further taken up for an extensive study.
14 citations
Cites methods from "Synthesis and Characterization of s..."
...The total cell protein content was determined by sulphoradamine B (SRB) assay [19]....
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TL;DR: Cytotoxicity of gamma linolenic acid and stearic acid analogues showed comparable cytotoxicity against the human lung carcinoma A-549 cell lines.
Abstract: Background
Preparation of some novel heterocyclic compounds with long alkyl and alkenyl chain of cytotoxic activity.
13 citations
Cites methods from "Synthesis and Characterization of s..."
...The total cell protein content was determined by Sulphoradamine B (SRB) assay [12,13]....
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