chiniofon has been researched along with Carcinoma--Ehrlich-Tumor* in 4 studies
4 other study(ies) available for chiniofon and Carcinoma--Ehrlich-Tumor
| Article | Year |
|---|---|
Elucidation of structure-activity relationship of 2-quinolone derivatives and exploration of their antitumor potential through Bax-induced apoptotic pathway.
3-Aryl-2-quinolone derivates were extensively investigated for their inhibition of farnesyl transferase. Taking this as a cue, we studied the other possible mechanism of antitumor activity of 2-quinolone derivates. A series of new 2-quinolone derivatives have been synthesized and screened for their cytotoxicity by trypan blue assay on Ehrlich ascites carcinoma cells and MTT assay on MCF-7 cells. Compound 1a (nJST) was found to be more effective in both studies with the lowest CTC(50) value among all nine synthesized compounds. This compound was further screened on four different cell lines, viz. human breast adenocarcinoma (MCF-7, MDA-MB-231), colon cancer (HCT-15), murine melanoma (B16F10) cell lines for 24 and 48 h. The CTC(50) value of the compound was found to be <10 μm. Compound 1a induced DNA damage which was revealed by DNA fragmentation studies and further confirmed by nuclear staining. The compound also showed significant elevation in Bax and reduction Bcl-2 gene expression levels. Acute toxicity study in mice indicated that the compound is safe till 2000 mg/kg. Two different doses 50 and 100 mg/kg were selected and studied in Ehrlich ascites carcinoma model of cancer and have shown significant improvement in survival time and hematological parameters. Topics: Animals; Antineoplastic Agents; Apoptosis; bcl-2-Associated X Protein; Breast Neoplasms; Carcinoma, Ehrlich Tumor; Cell Line, Tumor; Cell Survival; DNA Fragmentation; Female; Gene Expression Regulation, Neoplastic; Humans; Hydroxyquinolines; Mice; Neoplasms; Quinolones | 2012 |
7-substituted-4-hydroxyquinoline-3-carboxylic acids as inhibitors of dehydrogenase enzymes and of the respiration of Ehrlich ascites tumor cells: multivariate analysis and quantitative structure-activity relationship for polar substituents.
The inhibitory activities of a set of nine 7-substituted-4-hydroxyquinoline-3-carboxylic acids against three dehydrogenase enzymes and one whole cell system (Ehrlich ascites tumor cells) have been subjected to principal component analysis. The results clearly indicate that activity against the whole cell test system cannot directly be attributed to inhibition of the enzymes evaluated. The enzyme systems are reflected by the first component that can be identified with polar and steric parameters while hydrophobic effects are absent. The second component is entirely due to the inhibition of ascites cell respiration that depends primarily on hydrophobicity. Topics: Analysis of Variance; Animals; Carboxylic Acids; Carcinoma, Ehrlich Tumor; Hydroxyquinolines; L-Lactate Dehydrogenase; Malate Dehydrogenase; Oxygen Consumption; Solubility; Structure-Activity Relationship | 1985 |
4-hydroxyquinoline-3-carboxylic acids as inhibitors of cell respiration. 2. Quantitative structure-activity relationship of dehydrogenase enzyme and Ehrlich ascites tumor cell inhibitions.
Studies on dehydrogenase enzyme inhibition have been extended with the design, synthesis, and correlation analysis of 7-[(substituted-benzyl)oxy]-, 7-[(substituted-phenethyl)oxy]-, and 7([substituted-phenoxy)ethoxy]-4-hydroxyquinoline-3-carboxylic acids. Sixteen new congeners and the fifteen molecules previously synthesized have been tested against cytoplasmic malate dehydrogenase and lactate dehydrogenase, as well as against mitochondrial malate dehydrogenase. The lipophilic congeners show a clear specificity for inhibition of the mitochondrial enzyme. Correlation analysis of the data on the three enzymes allows a comparison of the binding sites in quantitative terms, while examination of the data on inhibition of ascites tumor cell respiration affords an indication of membrane transport. A newly developed high-pressure liquid chromatography based retention index is compared to the octanol-water pi constant as a model for hydrophobic interactions. Topics: Animals; Antineoplastic Agents; Carcinoma, Ehrlich Tumor; Hydroxyquinolines; L-Lactate Dehydrogenase; Malate Dehydrogenase; Oxygen Consumption; Rabbits; Structure-Activity Relationship | 1982 |
Design, synthesis, and correlation analysis of 7-substituted 4-hydroxyquinoline-3-carboxylic acids as inhibitors of cellular respiration.
Fifteen 7-substituted 4-hydroxyquinoline-3-carboxylic acids have been designed to minimize covariance between the physicochemical substituent parameters: pi, MR, and sigmap. The molecules have been synthesized and evaluated for their ability to inhibit the respiration of Ehrlich ascites cells as a whole cell model and for their ability to inhibit malate dehydrogenase as an intracellular target enzyme model. Correlation analysis indicates that ascites cell inhibition is linearly related to pi and that malate dehydrogenase inhibition is linearly related to MR. Topics: Animals; Carcinoma, Ehrlich Tumor; Cells, Cultured; Depression, Chemical; Hydroxyquinolines; In Vitro Techniques; Malate Dehydrogenase; Oxygen Consumption; Regression Analysis; Structure-Activity Relationship | 1977 |