Novel Tri-substituted Thiazoles Bearing Piperazine Ring: Synthesis and Evaluation of their Anticancer Activity

2019 ◽  
Vol 16 (5) ◽  
pp. 547-555 ◽  
Author(s):  
Asaf Evrim Evren ◽  
Leyla Yurttaş ◽  
Busra Eksellı ◽  
Gulsen Akalın-Cıftcı

Background: Cancer cells are described as an unregulated growth and spread of abnormal cells. Recently, cancer has become the most important major reason for deaths in the world. Methods: For anticancer activity, we have used the MTT method and determine the early/late apoptosis by flow cytometry. Results: The title compounds were procured by reacting 2-chloro-N-[4-(pyridin-4-yl)thiazol-2- yl]acetamide with some substituted piperazine derivatives. The in vitro anticancer activity of synthesized compounds was tested against C6 rat glioma cells and A549 human lung carcinoma cells. As a result, the compounds 3d, 3e, 3f and 3g have shown anticancer activity against both cell line. Conclusion: Specifically, compound 3f was determined as the most active compound against C6 rat glioma cells. Also, as understood, the core structure which is substituted with piperazine bridge, the heterocyclic aromatic derivatives are more active than phenyl or benzyl derivatives.

1970 ◽  
Vol 1 (1) ◽  
Author(s):  
TIAN Rui-rui

Objective: To investigate the effects of different concentrations of isorhamnetin on C6 rat glioma cells in vitro from January 2015 to June 2015. Methods: The blank control group, blank solvent control group and four concentration groups were used to observe the cell growth status under a microscope. MTT colorimetric assay was used to detect the effect of isorhamnetin on C6 glioma cells in vitro and the cell inhibition rate And survival rate were measured. The apoptotic and apoptotic rates were measured by flow cytometry in the treatment group and the control group. The relationship between the different concentrations of isorhamnetin and C6 glioma cell apoptosis was analyzed the total protein was extracted and the total AKT protein and Ser473 AKT protein content were detected by Western blotting. The rat model of glioma was constructed by SD rats.Five days of isorhamnetin was continuously fed and the plasma was detected by high-performance liquid chromatography,liver, brain tissue isorhamnetin content. 


2015 ◽  
Vol 10 (4) ◽  
pp. 759 ◽  
Author(s):  
Bin Zhou ◽  
Qiang Fu ◽  
Sha-Sha Song ◽  
Hong-Li Zheng ◽  
Yu-Zhen Wei

<p class="Abstract">The aim of this study was to examine the anticancer effects of schizophyllan (a -D-glucan) against the growth of rat CNS-1 glioma cells and preliminarily assess its effect on inducing apoptosis and blocking cell cycle. In order to evaluate its inhibitory effect, firstly MTT assay was conducted followed by annexin V/propidium iodide double staining or propidium iodide single staining, apoptosis and cell cycle using flow cytometry. All the experiments were carried in a dose- and time-dependent manner. Experimental results showed that treatment of 40 and 60 mg/L schizophyllan significantly increa-sed the apoptotic rate and blocked the cell cycle. In addition, increase in the proportion of cells in G0/G1 phase and decrease in the proportion of S-phase cells were also observed. Overall experimental studies suggest that schizo-phyllan can significantly inhibit the growth of rat CNS-1 glioma cells, in vitro and induced apoptosis and blocked the cell cycle.</p><p> </p>


2018 ◽  
Vol 1 (1) ◽  
Author(s):  
Shumin Liang ◽  
Yijun Chen ◽  
Kaifei Wang

Objectives: To establish a simple, reliable, stable rat C6 glioma model, and to provide an operating platform for studying the pathogenesis and prevention and treatment of glioma. Methods: C6 rat glioma cells were cultured in vitro and cultured in the right caudate putamen of SD rats. After implantation, the survival status of rats was observed and the pathological sections were made. HE is dyeing under light microscope. Results: After 6 days of inoculation of C6 glioma cells, the survival status was good at about 7 days, and the intracranial hypertension was more obvious at about 14 days. Most of them were in the endangered state. In the 18 specimens of the rats, except for the accidental death, the other tumor formation rate was 75%. The tumor structure was obviously displaced with the prolongation of the age of the tumor. HE staining was used to observe the formation of glioma in rat brain. Conclusion: The animal model of C6 glioma is reliable and stable. Its tumor growth characteristics and pathological features are similar to those of human glioma, which can be used as an ideal model for clinical study of glioma.


2013 ◽  
Vol 8 (2) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Deepali Katoch ◽  
Dharmesh Kumar ◽  
Upendra Sharma ◽  
Neeraj Kumar ◽  
Yogendra S. Padwad ◽  
...  

Zephgrabetaine (1), a new betaine type Amaryllidaceae alkaloid, along with seven known alkaloids, lycorine, galanthine, lycoramine, hamayne, haemanthamine, tortuosine, and ungeremine were isolated from the bulbs of Zephyranthes grandiflora and their structures elucidated by spectroscopic data analysis. The isolated alkaloids were tested for in vitro cytotoxic activities against two cell lines, C-6 (rat glioma cells) and CHO-K1 (Chinese hamster ovary cells). A dose dependent cytotoxic effect was exhibited by all the alkaloids on these two cancer cell lines with prominent activity of lycorine and haemanthamine.


2015 ◽  
Vol 17 (suppl 5) ◽  
pp. v44.3-v44
Author(s):  
Viveka Nand Yadav ◽  
Gregory J. Baker ◽  
Daniel A. Orringer ◽  
Jason A. Heth ◽  
Shawn Hervey-Jumper ◽  
...  

2006 ◽  
Vol 5 (1) ◽  
pp. 20-28 ◽  
Author(s):  
Patrick B. Senatus ◽  
Yin Li ◽  
Christopher Mandigo ◽  
Gwen Nichols ◽  
Gaetan Moise ◽  
...  
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