Synthesis and structure–activity relationships of novel 1-arylmethyl-3-aryl-1H-pyrazole-5-carbohydrazide derivatives as potential agents against A549 lung cancer cells

2007 ◽  
Vol 15 (22) ◽  
pp. 6893-6899 ◽  
Author(s):  
Yong Xia ◽  
Zhi-Wu Dong ◽  
Bao-Xiang Zhao ◽  
Xiao Ge ◽  
Ning Meng ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cancer Cells ◽  
Lung Cancer Cells ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
A549 Lung

scholarly journals Structure–Activity Relationships and Molecular Docking Analysis of Mcl-1 Targeting Renieramycin T Analogues in Patient-derived Lung Cancer Cells

Cancers ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 875 ◽  
Author(s):  
Korrakod Petsri ◽  
Masashi Yokoya ◽  
Sucharat Tungsukruthai ◽  
Thanyada Rungrotmongkol ◽  
Bodee Nutho ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Molecular Docking ◽  
Cancer Cells ◽  
Benzene Ring ◽  
Lung Cancer Cells ◽  
Docking Analysis ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Anti Cancer ◽  
Molecular Docking Analysis

Myeloid cell leukemia 1 (Mcl-1) and B-cell lymphoma 2 (Bcl-2) proteins are promising targets for cancer therapy. Here, we investigated the structure–activity relationships (SARs) and performed molecular docking analysis of renieramycin T (RT) and its analogues and identified the critical functional groups of Mcl-1 targeting. RT have a potent anti-cancer activity against several lung cancer cells and drug-resistant primary cancer cells. RT mediated apoptosis through Mcl-1 suppression and it also reduced the level of Bcl-2 in primary cells. For SAR study, five analogues of RT were synthesized and tested for their anti-cancer and Mcl-1- and Bcl-2-targeting effects. Only two of them (TM-(–)-18 and TM-(–)-4a) exerted anti-cancer activities with the loss of Mcl-1 and partly reduced Bcl-2, while the other analogues had no such effects. Specific cyanide and benzene ring parts of RT’s structure were identified to be critical for its Mcl-1-targeting activity. Computational molecular docking indicated that RT, TM-(–)-18, and TM-(–)-4a bound to Mcl-1 with high affinity, whereas TM-(–)-45, a compound with a benzene ring but no cyanide for comparison, showed the lowest binding affinity. As Mcl-1 helps cancer cells evading apoptosis, these data encourage further development of RT compounds as well as the design of novel drugs for treating Mcl-1-driven cancers.

Targeted delivery of doxorubicin to A549 lung cancer cells by CXCR4 antagonist conjugated PLGA nanoparticles

2014 ◽  
Vol 88 (2) ◽  
pp. 529-538 ◽  
Author(s):  
Chuda Chittasupho ◽  
Kriengsak Lirdprapamongkol ◽  
Prartana Kewsuwan ◽  
Narong Sarisuta
Keyword(s):  
Lung Cancer ◽  
Cancer Cells ◽  
Targeted Delivery ◽  
Plga Nanoparticles ◽  
Lung Cancer Cells ◽  
Cxcr4 Antagonist ◽  
A549 Lung

Moringa oleifera: Natural leaf extract with potential anti-cancerous effect on A549 lung cancer cells

Lung Cancer ◽  
2012 ◽  
Vol 77 ◽  
pp. S22 ◽  
Author(s):  
M. Dany ◽  
N. Madi ◽  
N. Nemer ◽  
M. Beyrouthy ◽  
S. Abdoun ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cancer Cells ◽  
Leaf Extract ◽  
Moringa Oleifera ◽  
Lung Cancer Cells ◽  
Natural Leaf ◽  
A549 Lung

Quercetin metabolites inhibit MMP-2 expression in A549 lung cancer cells by PPAR-γ associated mechanisms

2016 ◽  
Vol 33 ◽  
pp. 45-53 ◽  
Author(s):  
Cheng-Hung Chuang ◽  
Chiao-Lin Yeh ◽  
Shu-Lan Yeh ◽  
En-Shyh Lin ◽  
Li-Yu Wang ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cancer Cells ◽  
Lung Cancer Cells ◽  
Ppar Γ ◽  
A549 Lung
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