Design, Synthesis and Screening Studies of Potent Thiazol-2-Amine Derivatives as Fibroblast Growth Factor Receptor 1 Inhibitors

2014 ◽  
Vol 14 (17) ◽  
pp. 2031-2041 ◽  
Author(s):  
B.V.S. Kumar ◽  
Narasu Lakshmi ◽  
M. Kumar ◽  
Gundla Rambabu ◽  
Thimmappa Manjashetty ◽  
...  
Keyword(s):  
Growth Factor ◽  
Fibroblast Growth Factor ◽  
Fibroblast Growth Factor Receptor ◽  
Growth Factor Receptor ◽  
Fibroblast Growth ◽  
Design Synthesis

Design, synthesis and biological evaluation of novel FGFR inhibitors bearing an indazole scaffold

2015 ◽  
Vol 13 (28) ◽  
pp. 7643-7654 ◽  
Author(s):  
Jian Liu ◽  
Xia Peng ◽  
Yang Dai ◽  
Wei Zhang ◽  
Sumei Ren ◽  
...  
Keyword(s):  
Growth Factor ◽  
Cancer Therapy ◽  
Fibroblast Growth Factor ◽  
Fibroblast Growth Factor Receptor ◽  
Growth Factor Receptor ◽  
Biological Evaluation ◽  
Fibroblast Growth ◽  
Design Synthesis ◽  
Potential Target ◽  
Synthesis And Biological Evaluation

Fibroblast growth factor receptor (FGFR) is a potential target for cancer therapy.

scholarly journals Design, Synthesis and Biological Evaluation of 6-(2,6-dichloro-3,5-dimethoxyphenyl)-4-Substituted-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors

2016 ◽  
Author(s):  
Zhen Zhang ◽  
Dongmei Zhao ◽  
Yang Dai ◽  
Maosheng Cheng ◽  
Meiyu Geng ◽  
...  
Keyword(s):  
Growth Factor ◽  
Fibroblast Growth Factor ◽  
Fibroblast Growth Factor Receptor ◽  
Growth Factor Receptor ◽  
Biological Evaluation ◽  
Fibroblast Growth ◽  
Design Synthesis ◽  
Promising Target ◽  
Cancer Types ◽  
Synthesis And Biological Evaluation

Tyrosine kinase fibroblast growth factor receptor (FGFR), which is aberrant in various cancer types, is a promising target for cancer therapy. Here we reported the design, synthesis, and biological evaluation of a new series of 6-(2,6-dichloro-3,5-dimethoxyphenyl)-4-substituted-1H-indazoles derivatives as potent FGFR inhibitors. Compound 10a was first identified as a potent FGFR1 inhibitor, with good enzymatic inhibition. Further structure-based optimization revealed that compound 13a is the most potent FGFR1 inhibitor in this series with the enzyme inhibitory activity about 30.2 nM of IC50 value.

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