Design, synthesis and inhibitory activity of novel 2, 3-dihydroquinolin-4(1H)-one derivatives as potential succinate dehydrogenase inhibitors

2021 ◽  
Vol 214 ◽  
pp. 113246
Author(s):  
Wei Cheng ◽  
Yingkun Yan ◽  
Tingting Xiao ◽  
Guilan Zhang ◽  
Tingting Zhang ◽  
...  
Keyword(s):  
Succinate Dehydrogenase ◽  
Inhibitory Activity ◽  
Design Synthesis ◽  
Succinate Dehydrogenase Inhibitors

Design, Synthesis, and Fungicidal Evaluation of Novel Pyrazole-furan and Pyrazole-pyrrole Carboxamide as Succinate Dehydrogenase Inhibitors

2017 ◽  
Vol 65 (26) ◽  
pp. 5397-5403 ◽  
Author(s):  
Ting-Ting Yao ◽  
Dou-Xin Xiao ◽  
Zhong-Shan Li ◽  
Jing-Li Cheng ◽  
Shao-Wei Fang ◽  
...  
Keyword(s):  
Succinate Dehydrogenase ◽  
Design Synthesis ◽  
Succinate Dehydrogenase Inhibitors

Design, Synthesis, Molecular Docking and Biological Evaluation of 1-(benzo[d]thiazol-2-ylamino)(phenyl)methyl)naphthalen-2-ol Derivatives as Antiproliferative Agents

2019 ◽  
Vol 16 (10) ◽  
pp. 837-845
Author(s):  
Sandhya Jonnala ◽  
Bhaskar Nameta ◽  
Murthy Chavali ◽  
Rajashaker Bantu ◽  
Pallavi Choudante ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Inhibitory Activity ◽  
Chinese Hamster Ovary Cells ◽  
Chinese Hamster ◽  
Mouse Skin ◽  
Coupling Reaction ◽  
Binding Mode ◽  
Biological Evaluation ◽  
Design Synthesis

A class of 1-((benzo[d]thiazol-2-ylamino)(phenyl)methyl)naphthalen-2-ol derivatives (4a-t) has been synthesized in good yields through a three component coupling reaction. The newly synthesized compounds were evaluated for their in vitro antiproliferative activity against five cell lines such as DU145 (human prostate cancer), MDA-MB-B231 (human breast cancer), SKOV3 (human ovarian cancer), B16-F10 (mouse skin melanoma) and CHO-K1 (Chinese hamster ovary cells), a noncancerous cell line. In vitro inhibitory activity indicates that compounds 4a, 4b, 4c, 4d, 4g, 4j, and 4o exhibited potent anti-proliferative behavior. Among them, compounds 4g, 4j and 4o found to be the most active members exhibiting remarkable growth inhibitory activity. Molecular docking facilitates to investigate the probable binding mode and key active site interactions in tubulins α and β proteins. The docking results are complementary to experimental results.

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