Synthesis and anti‐proliferation activity evaluation of novel 2‐chloroquinazoline as potential EGFR‐TK inhibitors

2021 ◽  
Author(s):  
Quan Zheng ◽  
Xuan-Bo Xu ◽  
Hao Jin ◽  
Wen Zhang ◽  
Guo-Wu Rao
Keyword(s):  
Activity Evaluation ◽  
Proliferation Activity ◽  
Tk Inhibitors

Die Anämie bei malignen Tumorerkrankungen

1989 ◽  
Vol 28 (06) ◽  
pp. 247-254
Author(s):  
E. Aulbert
Keyword(s):  
Malignant Tumors ◽  
Gradient Centrifugation ◽  
Tumor Resection ◽  
Hemoglobin Concentration ◽  
Limiting Factor ◽  
Novikoff Hepatoma ◽  
Tumor Mass ◽  
Lysosomal Fraction ◽  
Proliferation Activity ◽  
Morris Hepatoma

The cellular uptake and lysosomal accumulation of 67Ga-labelled transferrin within tumors of different malignancy were examined using tissue fractionation and immunological techniques. As tumor models the slowly growing Morris hepatoma 5123C, the moderately growing Novikoff hepatoma and the fast and aggressive Yoshida hepatoma AH 130 were investigated. Isolation of subcellular fractions of tumor homogenates was performed by differential centrifugation and density-gradient centrifugation. The intracellular 67Gatransferrin was found to be highly concentrated within the purified lysosomes. The transferrin within the lysosomal fraction was identified by radial immunodiffusion technique using monospecific antiserum. The accumulation of 67Gatransferrin by the tumors resulted in a faster disappearance of 67Ga-transferrin from the blood. This loss of circulating 67Ga-transferrin correlated with the proliferation activity and the spread of the tumors. Since transferrin is indispensible for the utilization of iron by the heme-synthesizing red cell precursors, transferrin concentration in the blood is the limiting factor for the utilization of iron in hemoglobin synthesis. Thus, in a further series of experiments we investigated the development of anemia in tumor-bearing rats. With increasing tumor mass a progressive fall of hemoglobin concentration was found. The anemia was more severe in the faster growing Novikoff hepatoma than in the slowly growing Morris hepatoma. The most significant reduction of hemoglobin concentration was found in the very fast growing Yoshida hepatoma. After total tumor resection hemoglobin concentration and red blood cell count normalized completely within 6-8 weeks. We conclude from these data that the uptake of transferrin by the tumor cells results in a faster disappearance of transferrin from the blood. This loss of circulating transferrin correlates with tumor mass and proliferation activity and is one of the factors responsible for the anemia seen in patients with malignant tumors.

Die Anämie bei malignen Tumorerkrankungen

1989 ◽  
Vol 28 (05) ◽  
pp. 193-200 ◽  
Author(s):  
E. Aulbert
Keyword(s):  
Cellular Uptake ◽  
Tumor Tissue ◽  
Malignant Tumors ◽  
The Other ◽  
Novikoff Hepatoma ◽  
Cellular Accumulation ◽  
Tumor Mass ◽  
Proliferation Activity ◽  
Morris Hepatoma ◽  
Cellular Incorporation

Cellular uptake of 67Ga-labelled transferrin by the tumor tissue was studied in rats with tumors of different malignancy and different tumor mass using the slowly growing Morris hepatoma 5123C, the moderately growing Novikoff hepatoma and the very fast and aggressive Yoshida hepatoma AH130. The cellular accumulation of 67Ga-transferrin was found to correlate with the proliferation activity of the tumor. The 67Ga-transferrin concentration in the very fast growing Yoshida hepatoma was 4.8 times higher than the concentration in the slowly growing Morris hepatoma. The uptake of 67Ga-transferrin by the tumors resulted in a faster disappearance of circulating 67Ga-transferrin from the blood. The rate of disappearance correlated with the proliferation activity and the spread of the tumors. Using tumors of identical size the elimination of 67Ga-transferrin from the blood was much faster in the rats with Yoshida hepatoma than in those with the slowly growing Morris hepatoma. On the other hand, using tumors of different tumor size it could be demonstrated that the rate of disappearance of 67Ga-transferrin from the blood correlated directly with tumor mass. It is concluded that cellular incorporation of transferrin within the tumor cells results in a loss of circulating transferrin, which correlates with tumor mass and proliferation of tumor. This mechanism is supposed to be the cause for the hypotransferrinemia seen in patients with malignant tumors.

Synthesis, photosensitization and antimicrobial activity evaluation of some novel Merocyanine dyes

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Aspergillus Flavus ◽  
Elemental Analysis ◽  
Cyanine Dyes ◽  
Fungal Strains ◽  
Activity Evaluation ◽  
Visible Spectra ◽  
Merocyanine Dyes

Novel acyclic and cyclic merocyanine dyes derived from the nucleu of furo [(3,2-d) pyrazole; ( d 2 , 3 )imidazole]were prepared. The electronic visible absorptionspectra of all the synthesized new cyanine dyes were examined in 95% ethanolsolution to evaluate their photosensitization properties. Antibacterial andantifungal activities for some selected dyes were tested against various bacterialand fungal strains (Escherichia coli, Staphylococcus aureus, Aspergillus flavus andCandida albicans) to evaluate their antimicrobial activity. Structural identificationwas carried out via elemental analysis, visible spectra, IR and 1H NMRspectroscopic data.

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