scholarly journals Synthesis, in vitro anticancer and antioxidant activity of thiadiazole substituted thiazolidin-4-ones

2013 ◽  
Vol 63 (3) ◽  
pp. 397-408 ◽  
Author(s):  
Alex Joseph ◽  
Chaitanyakumar S. Shah ◽  
Suthar Sharad Kumar ◽  
Angel Treasa Alex ◽  
Naseer Maliyakkal ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Thioglycolic Acid ◽  
Aromatic Aldehydes ◽  
Breast Adenocarcinoma ◽  
Human Breast ◽  
Dpph Assay ◽  
Alkyl Aryl ◽  
Adenocarcinoma Cells ◽  
Mcf 7

Abstract A series of novel 5-alkyl/aryl thiadiazole substituted thiazolidin-4-ones were synthesized by a two-step process. In the first step, 5-alkyl/aryl substituted 2-aminothiadiazoles were synthesized, which on reaction with substituted aromatic aldehydes and thioglycolic acid in the presence of dicyclohexylcarbodiimide afforded thiazolidin- 4-ones. All the compounds were synthesized in fairly good yields and their structures were confirmed by spectral and physical data. The title compounds were screened for in vitro anti-proliferative activity on human breast adenocarcinoma cells (MCF-7) by MTT assay. Most of the derivatives showed an IC50 less than 150 μmol L-1. Among the compounds tested, 2-(2-nitrophenyl)- 3-(5-methyl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3f), 2-(3-fluorophenyl)-3-(5-methyl-1,3,4-thiadiazol-2- -yl)-thiazolidin-4-one (3b), and 2-(4-chlorophenyl)-3- -(5-methyl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3c) were found to be the most active derivatives with IC50 values of 46.34, 66.84, and 60.71 μmol L-1, respectively. Antioxidant studies of all the synthesized compounds were carried out by diphenylpicrylhydrazyl (DPPH) assay. Among the compounds tested, 2-phenyl-3-(5-styryl- -1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3s) elicited superior antioxidant activity with IC50 of 161.93 μmol L-1.

scholarly journals Preliminary phytochemical screening and anticancer potential of Kohautia aspera (Heyne Ex Roth) Bremek

2019 ◽  
Vol 10 (3) ◽  
pp. 2502-2506
Author(s):  
Kavitha G ◽  
Sivakkumar T ◽  
Elessy Abraham
Keyword(s):  
Breast Adenocarcinoma ◽  
Phytochemical Screening ◽  
Human Breast ◽  
Human Breast Adenocarcinoma ◽  
Percolation Method ◽  
Adenocarcinoma Cells ◽  
Successive Extraction ◽  
Potential Evaluation ◽  
Mcf 7

Phytochemical screening followed by anticancer potential evaluation of Kohautia aspera (Heyne ex Roth) Bremek was the purpose of the study. Successive extraction was performed with four solvents of different polarity as well as hot percolation method for the aqueous extract. The anticancer potential of the plant was investigated by standard MTT assay against (MCF-7) human breast adenocarcinoma cells. The extracts showed many phytoconstituents. In vitro cytotoxic activity of plant increased with increasing concentration of extracts. The presence of important phytoconstituents in plants may provide protection against a number of diseases. The investigation concludes that Kohautia aspera (Heyne ex Roth) Bremek possesses significant anticancer potential.

scholarly journals Change in the Expression of BAK، FAS، BAX، TNF-A، BCL-2 and Survivin Apoptosis Genes of the Human Breast Adenocarcinoma Cells (MCF-7) by Staphylococcal Enterotoxin B

2019 ◽  
Author(s):  
Sara Afzali ◽  
Abbas Doosti ◽  
Mansour Heidari ◽  
Nahid Babaei ◽  
Parvaneh Keshavarz
Keyword(s):  
Staphylococcal Enterotoxin ◽  
Breast Adenocarcinoma ◽  
Control Group ◽  
Staphylococcal Enterotoxin B ◽  
Type B ◽  
Human Breast ◽  
Human Breast Adenocarcinoma ◽  
Adenocarcinoma Cells ◽  
Enterotoxin B ◽  
Mcf 7

Introduction: Breast cancer is one of the most prevalent malignancies among women. Patients whose suffering from this condition, as a result of the use of conventional therapies often have a poor response to treatment and the relapse among them is frequent. In this study, the effects of staphylococcal enterotoxin type B on BAK، FAS، BAX، TNF-a، BCL-2 و Survivin genes expression in human breast adenocarcinoma cells (MCF-7) was examined. Staphylococcal enterotoxin B is a powerful member of the Staphylococcus aureus toxins family, which is known as an anticancer agent with potential for killing cancer cells. Methods: The experimental study was carried out at the Biotechnology Research Center of Islamic Azad University, Shahrekord Branch. By using Lipofectamine 2000 reagent, MCF-7  cells transfected with the pcDNA3.1(+)-seb (recombinant) and  pcDNA3.1(+) (non-recombinant)  plasmids and were selected by culturing in a selective medium of RPMI- 1640 containing 600 μg / mL antibiotic G418. Then, the expression of BAK, FAS, BAX, TNF-a, BCL-2, and Survivin genes in transfected cells were analyzed by real time PCR. Student's t-test, SPSS Inc., Chicago, IL; Version 16 and also Excel program for statistical analysis were used. Results: The results of this study indicated that staphylococcal enterotoxin type B (SEB) remarkably changes the expression of apoptotic related genes in MCF-7 cell line. It was observed a significant increase in the expression of BAK, FAS, BAX, and TNF-a genes, the expression of BCL-2 and Survivin genes significantly decreased compared to the control group (P=0/032). Conclusion: Staphylococcal enterotoxin type B has an inhibitory effect on the growth, proliferation and invasion of breast adenocarcinoma cells through altering the expression of the genes involved in the apoptosis process. Therefore, it seems that there is a good research field for the use of this toxin in the control and treatment of human breast adenocarcinoma.

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.

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