scholarly journals Pro‑apoptotic activity of novel synthetic isoxazole derivatives exhibiting inhibitory activity against tumor cell growth in vitro

2020 ◽  
Vol 20 (5) ◽  
pp. 1-1
Author(s):  
Ilaria Lampronti ◽  
Daniele Simoni ◽  
Riccardo Rondanin ◽  
Riccardo Baruchello ◽  
Chiara Scapoli ◽  
...  
Keyword(s):  
Cell Growth ◽  
Tumor Cell ◽  
Inhibitory Activity ◽  
Tumor Cell Growth ◽  
Apoptotic Activity ◽  
Isoxazole Derivatives

scholarly journals Synthesis of Novel Pyrazole Derivatives and Their Tumor Cell Growth Inhibitory Activity

Molecules ◽  
2019 ◽  
Vol 24 (2) ◽  
pp. 279 ◽  
Author(s):  
Ying-Jie Cui ◽  
Long-Qian Tang ◽  
Cheng-Mei Zhang ◽  
Zhao-Peng Liu
Keyword(s):  
Cell Growth ◽  
Tumor Cell ◽  
Inhibitory Activity ◽  
Lung Tumor ◽  
A549 Cells ◽  
Phenyl Isothiocyanate ◽  
Pyrazole Derivatives ◽  
Tumor Cell Growth ◽  
Growth Inhibitory ◽  
Mcf 7

To find novel antitumor agents, a series of 1H-benzofuro[3,2-c]pyrazole derivatives 4a-e were designed and synthesized. The treatment of 6-methoxybenzofuran-3(2H)-one 3 with LiHMDS in anhydrous tetrahydrofuran (THF) followed by reaction with 3-substitued phenyl isothiocyanate gave the thioamide intermediates, which underwent condensation with hydrazine monohydrate in dioxane/EtOH (1:1) to provide the benzofuropyrazole derivatives 4a–e as well as the unexpected pyrazole derivatives 5a–e. In tumor cell growth inhibitory assay, all the benzofuropyrazole derivatives were not active against the breast tumor MCF-7 cell, only 4a was highly active and more potent than ABT-751 against the leukemia K562 (GI50 = 0.26 μM) and lung tumor A549 cells (GI50 = 0.19 μM), while other benzofuropyrazoles showed very weak inhibitory activity. In contrast, the pyrazoles 5a-e were in general more potent than the benzofuropyrazoles 4a–e. Compound 5a exhibited a similar tendency to that of 4a with high potency against K562 and A549 cells but weak effects on MCF-7 cell. Both pyrazoles 5b and 5e exhibited high inhibitory activities against K562, MCF-7 and A549 cells. The most active compound 5b was much more potent than ABT-751 against K562 and A549 cells with GI50 values of 0.021 and 0.69 M, respectively. Moreover, 5b was identified as a novel tubulin polymerization inhibitor with an IC50 of 7.30 M.

Abstract 1914: A novel celecoxib derivative that lacks COX-2 inhibition but displays potent colon tumor cell growth and PDE5 inhibitory activity

2015 ◽  
Author(s):  
Sara C. Sigler ◽  
Veronica Ramirez-Alcantara ◽  
Adam B. Keeton ◽  
Mohammad Abdel-Halim ◽  
Ashraf H. Abadi ◽  
...  
Keyword(s):  
Cell Growth ◽  
Tumor Cell ◽  
Inhibitory Activity ◽  
Colon Tumor ◽  
Tumor Cell Growth ◽  
Colon Tumor Cell ◽  
Cox 2
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