scholarly journals Synthesis and Bioevaluation of Thieno[2,3-d]pyrimidinone Derivatives as Potential Tumor Cell Growth Inhibitors

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Huangyong Li ◽  
Changshui Chen ◽  
Shengzhen Xu ◽  
Xiufang Cao
Keyword(s):  
Cell Growth ◽  
Tumor Cell ◽  
Bioactive Molecules ◽  
Tumor Cell Growth ◽  
Growth Inhibitors ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Inhibitory Activities ◽  
Alkylation Reactions ◽  
Mcf 7

A series of novel cycloalkylthieno[2,3-d]pyrimidinone derivatives have been conveniently synthesizedviathree steps including G-3CR, heterocyclization, and alkylation reactions as a part of our ongoing search for new bioactive molecules. The newly synthesized compounds were evaluated for their potential tumor cell growth inhibitory activity by standard MTT assay. The preliminary results show that compound6bexhibited better inhibitory activities against HepG2, MCF-7, and BCG-823 cell lines compared to the control.

Synthesis of a Natural Chalcone and Its Prenyl Analogs - Evaluation of Tumor Cell Growth-Inhibitory Activities, and Effects on Cell Cycle and Apoptosis

2012 ◽  
Vol 9 (6) ◽  
pp. 1133-1143 ◽  
Author(s):  
Marta P. Neves ◽  
Raquel T. Lima ◽  
Kanthima Choosang ◽  
Panee Pakkong ◽  
Maria de São José Nascimento ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Growth ◽  
Tumor Cell ◽  
Tumor Cell Growth ◽  
Growth Inhibitory ◽  
Inhibitory Activities

Farnesyl protein transferase and tumor cell growth inhibitory activities of lipiferolide isolated fromLiriodendron tulipifera

2007 ◽  
Vol 30 (3) ◽  
pp. 299-302 ◽  
Author(s):  
Mi Kyeong Moon ◽  
Hyun Mi Oh ◽  
Byoung-Mog Kwon ◽  
Nam-ln Baek ◽  
Sung-Hoon Kim ◽  
...  
Keyword(s):  
Cell Growth ◽  
Tumor Cell ◽  
Tumor Cell Growth ◽  
Growth Inhibitory ◽  
Farnesyl Protein Transferase ◽  
Inhibitory Activities

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.

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