scholarly journals Synthesis, Biological Evaluation and Docking Study of Etodolac-Triazole Conjugate

Author(s):  
Papigani Neeraja ◽  
Suryapeta Srinivas ◽  
Venkanna Banothu ◽  
Khagga Mukkanti ◽  
Pramod Kumar Dubey ◽  
...  

A new set of 15 compounds containing etodolac moiety and triazole ring were prepared by CuAAC reaction in moderate to high yield. All the synthesized compounds were purified by chromatographic techniques and characterized by spectral data IR, 1H and 13C NMR and mass spectrometry. The newly derived compounds were screened for their anti-bacterial activities against one gram-positive (S. aureus) and two gram-negative (E. coli, K. pneumoniae) bacteria using an agar-well diffusion method. Most of the compounds showed good to moderate antibacterial activities. Especially compound 4e having good activities against all the strains. The compound 4e displayed significant inhibitory potential with MIC 25 µg/mL against all the strains. The potential DNA gyrase inhibitory activity of this compound was investigated by using molecular docking studies carried out using Autodock Vina software. The compound 4e showed the lowest ΔGbind results (-7.7 Kcal/mol, -7.9Kcal/mol). The cytotoxic activity of the obtained compounds was determined using A549 cancer cell line by a MTT assay. They displayed promising activity against the human lung cancer cell line. Especially 4o, 4b, 4d shown lowest IC50 values.

2011 ◽  
Vol 31 (10) ◽  
pp. 1091-1095
Author(s):  
Xiao-lin LI ◽  
Yan-fang ZHANG ◽  
Kai TANG ◽  
Ying TANG ◽  
Ruo-bing JIN ◽  
...  

Author(s):  
M. Afrin Nisha ◽  
S. Preetha ◽  
J. Selvaraj ◽  
G. Sridevi

Background: Kabasura kudineer is widely known for its anticancer efficiency. Kabasura kudineer is a customary formulation used by siddha practitioners for effectively managing common respiratory illness. Herbal medicines are acknowledged as a great approach to lung cancer therapy. Aim of the study is to know about the anticancer property of Kabasura kudineer extract on inflammatory cytokines IL-6 and TNF-α in lung cancer cell line (A549). Materials and Methods: Human lung cancer cell line (A549) was purchased from National Centre for Cell Sciences (NCCS), Pune, India. Cell viability test was done by MTT assay. Gene expression analysis was done by Real Time-PCR. The obtained data were analysed statistically by one-way analysis of variance and Duncan’s multiple range test with Graph Pad Prism version 5 to analyse the significance. The significance was considered at p<0.05 level in Duncan’s test. Results and Discussion: Kabasura kudineer caused a marked increase in cell death in dose dependent manner. AT the end of 48 hours, maximum inhibition was at 400 and 500 μg/ml. Kabasura kudineer extract reduced the expression of IL-6 and TNF-α compared to the control cells. Conclusion: This study concluded that Kabasura kudineer extract has anticancer activity on lung cancer cell lines (A549).


2012 ◽  
Vol 66 (6) ◽  
pp. 439-447 ◽  
Author(s):  
Yang Song ◽  
Liyan Xue ◽  
Sha Du ◽  
Mingzhong Sun ◽  
Jun Hu ◽  
...  

Molecules ◽  
2016 ◽  
Vol 21 (10) ◽  
pp. 1267 ◽  
Author(s):  
Zheng Wang ◽  
Xue Wu ◽  
Yan-Ni Liang ◽  
Li Wang ◽  
Zhong-Xing Song ◽  
...  

2009 ◽  
Vol 66 (3) ◽  
pp. 178
Author(s):  
Joo Han Song ◽  
Eun Joo Jeon ◽  
Hee Won Kwak ◽  
Hye Min Lee ◽  
Sung Gun Cho ◽  
...  

2020 ◽  
Vol 24 ◽  
pp. 101525 ◽  
Author(s):  
Gopal Suresh ◽  
Dhanasegaran Kokila ◽  
Thirunavukarasu Chitrikha Suresh ◽  
Subramanian Kumaran ◽  
Palanivel Velmurugan ◽  
...  

2015 ◽  
Vol 14 (2) ◽  
pp. 4005-4014 ◽  
Author(s):  
G.M. Chen ◽  
R.F. Ding ◽  
Y.D. Tan ◽  
X.B. Pan ◽  
G.M. Jiang ◽  
...  

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