scholarly journals 3-{[(2,3-Dichlorophenyl)amino]methyl}-5-(furan-2-ylmethylidene)-1,3-thiazolidine-2,4-dione

Molbank ◽  
10.3390/m1083 ◽  
2019 ◽  
Vol 2019 (4) ◽  
pp. M1083
Author(s):  
Uwabagira ◽  
Sarojini
Keyword(s):  
Breast Adenocarcinoma ◽  
Cyclin Dependent Kinase ◽  
Human Breast ◽  
Hemolysis Assay ◽  
Human Breast Adenocarcinoma ◽  
Inflammatory Agent ◽  
Human Blood Cell ◽  
Anti Inflammatory ◽  
Mcf 7

The compound 3-{[(2,3-Dichlorophenyl)amino]methyl}-5-(furan-2-ylmethylidene)-1,3-thiazolidine-2,4-dione has been designed, synthesized, and screened for its in vitro antibreast cancer activity, using human breast adenocarcinoma cell lines (MCF-7) and in vitro anti-inflammatory activity. By hemolysis assay, it showed that it has a nonhemolytic and nontoxic effect on human blood cell. The title compound 5, subjected to in vitro activities, showed that it is cytotoxic with an IC50 of 42.30 µM and a good anti-inflammatory agent. The docking results against cyclin dependent kinase 2 (CDK2) (PDB ID: 3QQK) gave insights on its inhibitory activity.

Photodynamic activity of 2,6-diiodo-3,5-dithienylvinyleneBODIPYs and their folate-functionalized chitosan-coated Pluronic® F-127 micelles on MCF-7 breast cancer cells

2020 ◽  
Vol 24 (05n07) ◽  
pp. 973-984
Author(s):  
Nthabeleng Molupe ◽  
Balaji Babu ◽  
David O. Oluwole ◽  
Earl Prinsloo ◽  
Lizhi Gai ◽  
...  
Keyword(s):  
Breast Cancer Cells ◽  
Drug Delivery Systems ◽  
Quantum Yields ◽  
Breast Adenocarcinoma ◽  
Human Breast ◽  
Human Breast Adenocarcinoma ◽  
Viable Cells ◽  
Photodynamic Activity ◽  
Mcf 7

A 2,6-diiodo-3,5-dithienylvinyleneBODIPY dye was prepared and encapsulated with folate-chitosan capped Pluronic[Formula: see text] F-127 to provide drug delivery systems for photodynamic therapy (PDT). Moderately enhanced singlet oxygen quantum yields were observed for the dye encapsulation complexes in water. The in vitro dark cytotoxicity and photodynamic activity were investigated on the human breast adenocarcinoma (MCF-7) cell line. Minimal dark cytotoxicity was observed for the BODIPY dyes in 5% DMSO and when encapsulated in folate-functionalized chitosan-coated Pluronic[Formula: see text] F-127 micelles, since the cell viability values are consistently greater than 80% over the 0-40 [Formula: see text] concentration range. Upon irradiation of the samples, significant cytocidal activity was observed for the encapsulation complex of a 2,6-diiodo-8-dimethylaminophenyl-3,5-dithienylvinyleneBODIPY dye with less than 50% viable cells observed at concentrations [Formula: see text].

DNA Adduct Formation by the Anticancer Drug Ellipticine and Its Hydroxy Derivatives in Human Breast Adenocarcinoma MCF-7 Cells

2004 ◽  
Vol 69 (3) ◽  
pp. 603-615 ◽  
Author(s):  
Lucie Bořek-Dohalská ◽  
Eva Frei ◽  
Marie Stiborová
Keyword(s):  
Breast Cancer ◽  
Cytochrome P450 ◽  
Cancer Cells ◽  
Dna Adducts ◽  
Breast Adenocarcinoma ◽  
Antitumor Action ◽  
Human Breast ◽  
Human Breast Adenocarcinoma ◽  
Mcf 7

The cytotoxicity of the antineoplastic agent ellipticine and its 9- and 7-hydroxylated metabolites to human breast adenocarcinoma MCF-7 cells and their ability to generate DNA adducts in these cancer cells were investigated. Ellipticine and its 9-hydroxylated metabolite were found to be toxic to MCF-7 cells with IC50 values of 1.25 and 3.25 μmol l-1 for ellipticine and 9-hydroxyellipticine, respectively. In contrast, no toxicity to these cancer cells was detectable for 7-hydroxyellipticine. The nuclease P1 version of the 32P-postlabeling assay yielded a pattern of ellipticine-DNA adducts with two major and one minor adducts in MCF-7 cells, similar to the pattern of adducts detected in DNA reacted with ellipticine and the reconstituted cytochrome P450 enzyme system in vitro and in DNA in vivo. The identity of two major adducts formed in DNA of MCF-7 cells with those formed by cytochrome P450-mediated ellipticine activation in vitro was confirmed by HPLC of the isolated adducts. 9-Hydroxyellipticine was also capable of inducing DNA adducts in MCF-7 cells, but to a lesser extent. In addition, the adducts generated by 9-hydroxyellipticine were different from those generated by ellipticine. Negligible levels of DNA adducts were detectable in DNA of MCF-7 cells exposed to 7-hydroxyellipticine. The results presented here are the first report showing the formation of covalent DNA adducts with ellipticine in human breast cancer cells in culture, and suggest the formation of covalent DNA adducts as a new mode of antitumor action of ellipticine in breast cancer.

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