scholarly journals Design, synthesis and biological evaluation of 1H-pyrrolo[2,3-b]pyridine derivatives as potent fibroblast growth factor receptor inhibitors

RSC Advances ◽  
2021 ◽  
Vol 11 (34) ◽  
pp. 20651-20661
Author(s):  
Xingping Su ◽  
Zhihao Liu ◽  
Lin Yue ◽  
Xiuli Wu ◽  
Wei Wei ◽  
...  
Keyword(s):  
Fibroblast Growth Factor Receptor ◽  
Growth Factor Receptor ◽  
Biological Evaluation ◽  
Fibroblast Growth ◽  
Pyridine Derivatives ◽  
Ligand Efficiency ◽  
Design Synthesis ◽  
New Class ◽  
Synthesis And Biological Evaluation ◽  
High Ligand

Discovery of a new class of 1H- pyrrorole [2,3-b]pyridine FGFR inhibitors with high ligand efficiency.

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.

scholarly journals Design, synthesis and biological evaluation of 2-aminopyrimidinones and their 6-aza-analogs as a new class of CK2 inhibitors

2013 ◽  
Vol 29 (5) ◽  
pp. 639-646 ◽  
Author(s):  
Maksym O. Chekanov ◽  
Olga V. Ostrynska ◽  
Sergii S. Tarnavskyi ◽  
Anatoliy R. Synyugin ◽  
Nadiia V. Briukhovetska ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
New Class ◽  
Synthesis And Biological Evaluation ◽  
Ck2 Inhibitors
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