scholarly journals Design, Syntheses and Antitumor Activities Evaluation of 1,5-diaryl Substituted Pyrazole Secnidazole Ester Derivatives

Author(s):  
Qing-Hu Teng ◽  
Gui-Xia Sun ◽  
Shu-Ying Luo ◽  
kai wang ◽  
Fu-Pei Liang

Abstract According to the drug hybridization principle, a series of novel 1,5-diaryl substituted pyrazole secnidazole ester derivatives (6aa-6gc) have been synthesized by the combinations of various 1,5-diarylpyrazole-3-carboxylic acids with secnidazole. The in vitro antitumor/cytotoxicities activities against tumor and normal cell lines, including NCI-H460 (lung tumor cell), MCG-803 (gastric tumor cell), Skov-3 (ovarian tumor cell), BEL-7404 (liver tumor cell) and HL-7702 (normal liver cell), have been evaluated using MTT assay. All compounds showed promising inhibitory activities against four tumor cell lines. The IC50 of 6bc against the BEL-7404 cell was 2.03 μM, and those of 6fc against the NCI-H460, MCG-803 and Skov-3 were 1.34, 0.14 and 0.87 μM, respectively. All these values were much lower than those of the cisplatin. Furthermore, 6fc and 6bc were also verified to be considerable safe for normal human liver cell, since the lower IC50 values than cisplatin. Based on these results, the cell cycle analysis, apoptosis ratio detection, and mitochondrial membrane potential assay of 6fc and 6bc were further performed aiming to investigate their inhibition mechanism of BEL-7404 cells. It is revealed that they have effectively inhibited the cell growth by arresting the BEL-7404 cells at S phase and induced apoptosis through the mitochondria-mediated pathway.

2001 ◽  
Author(s):  
Mohammad Islam ◽  
Norio Mitsuhashi ◽  
Tetsuo Akimoto ◽  
Hideyuki Sakurai ◽  
Masatoshi Hasegawa ◽  
...  

2020 ◽  
Vol 66 (5) ◽  
pp. 563-571
Author(s):  
Anna Danilova ◽  
N. Avdonkina ◽  
Ye. Gubareva ◽  
I. Baldueva ◽  
Anton Zozulya ◽  
...  

Circadian clock is a complex mechanism regulating many different physiological processes. Preclinical, epidemiological and clinical studies demonstrate association between circadian rhythms disruption and tumor initiation. Study of modulation of solid tumor cells biological properties through enhancement of clock mechanisms could attribute to the development of more effective chemo- and hormone therapy approaches. Aim: Evaluate the effects of ovarian and lung tumor cells synchronization with dexamethasone in vitro on cells sensitivity to cisplatin. Materials and methods: Metastatic ovarian cancer (n=3) and lung cancer (n=3) cell lines were obtained from patients tumors. Tumor cell cultivation was performed in accordance with the protocol. Artificial synchronization was performed with dexamethasone 200 nM introduction to the cell cultures. Doses of cisplatin used were 1.5 and 3.0 mg/ml. xCELLigence Real-Time Cell Analysis and Cell-IQ was used to measure proliferation and chemoresistance of tumor cells. Results: Each cell-line had individual morphological characteristics and proliferation parameters. Preliminary incubation with dexamethasone (2 h) had a stimulating effect on proliferation of all tumor cell lines (Slope min -4.3(0.3)хЕ ‘х10-3 - max 36.8(0.6)хЫх10'3, min 2.2(0.2)хЕ1х10'3- max 50.4(0.8)хЕ1х10'3), and increased their sensitivity to cisplatin (min -43(2.6)хЕ1х10-3 - max 57.5(0.6)хЕ1х10-3 и min -217,3(2,2) -1,9(0,1)хч-1х10-3 - max -1,9(0,1)хч'1х10'3, respectively. Conclusion: These results should be the platform for future studies of the interaction of clock mechanisms, cell cycle regulation and viability of tumor cells.


Author(s):  
R.E. Nordquist ◽  
R.E. Coalson ◽  
J.A. Mohr ◽  
E.R. Rhoades ◽  
J.J. Coalson ◽  
...  

Ultrastructural studies of pulmonary needle biopsies from patients with alveolar cell carcinoma (ACC) revealed the presence of a virus-like material in the nucleus and cytoplasm of tumor cells. Stinson et. al. reported the presence of filamentous virus-like particles in four of six cases in an ultrastructural study of ACC. In vitro studies by Coalson et. al. confirmed the presence of a biological agent and demonstrated that cell-free supernate from tumor cell cultures could induce cytopathic effect when applied to indicator cell lines. It was also shown in this report that tumor cell lines derived from this tumor produced the filterable biological agent until the 18-20 passage in culture. An extension of this investigation on the cell lines derived from ACC demonstrated that a unique antigen was associated with ACC tumor cells and that this antigenicity could be induced in indicator cell lines following treatment with cell free extracts.


2007 ◽  
Vol 19 (2) ◽  
pp. 94-99
Author(s):  
Zhi-jun Liu ◽  
Bin Wang ◽  
Zhi-yong Yan ◽  
Dong-meng Qian ◽  
Xu-xia Song ◽  
...  

Author(s):  
YASMINE Y ◽  
CAROLINE JEBA R

Objective: The objective of the study was to investigate the cytotoxic activity of hydroalcoholic extract of a polyherbal powder on Vero (normal kidney) and Chang (normal liver) cell lines. Methods: The cytotoxic effect was evaluated by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-tetrazolium bromide assay. It is commonly used colorimetric assay for assessing cell metabolic activity under specific conditions, indicates the number of viable cells. Results: According to the experimental results, the hydroalcoholic extract does not cause any toxicity on normal liver and kidney cell lines and LC50 values are ca lculated using LDP line software and found 776.73 μg/ml and 686.58 μg/ml. Conclusion: The hydroalcoholic extract of polyherbal churnam exhibited cell viability at higher concentrations. The results indicates investigated formulation does not causes any toxicity to the normal liver and kidney cells and found to be safe for human consumption. Further, toxicological and pharmacological evaluation is required to prove its safety and efficacy.


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