Design, synthesis and biological evaluation of pyrazolo3,4-

Xiaowei WU; Mengdi Dai; Rongrong Cui; Yulan Wang; Chunpu LI; Xia Peng; Jihui Zhao; Bao Wang; Yang Dai; Dan Feng; Tianbiao Yang; Hualiang Jiang; Meiyu Geng; Jing AI; Mingyue Zheng; Hong Liu

Return

Design, synthesis and biological evaluation of pyrazolo3,4-

Author: Xiaowei WU ¹ ; Mengdi DAI ² ; Rongrong CUI ³ ; Yulan WANG ¹ ; Chunpu LI ¹ ; Xia PENG ² ; Jihui ZHAO ¹ ; Bao WANG ¹ ; Yang DAI ² ; Dan FENG ¹ ; Tianbiao YANG ¹ ; Hualiang JIANG ¹ ; Meiyu GENG ² ; Jing AI ² ; Mingyue ZHENG ¹ ; Hong LIU ¹
Author Information

1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
2. Division of Anti-Tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
3. School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing 210023, China.
Publication Type:Journal Article
Keywords: Antitumor efficacy; BTK, brutons tyrosine kinase; CADD, computer-aided drug design; Covalent FGFR inhibitors; EGFR, epidermal growth factor receptor; FGFR, fibroblast growth factor receptor; GSH, glutathione; MAPK, mitogen-activated protein kinase; PI3K, phosphoinositide 3-kinase; PK, pharmacokinetics; PLCγ, phospholipase Cγ; Pyrazolo[3,4-d]pyridazinone; RTKs, receptor tyrosine kinases; SAR, structure−activity relationship; Structure−activity relationships; Tyrosine kinase; Virtual screening
From: Acta Pharmaceutica Sinica B 2021;11(3):781-794
CountryChina
Language:English
Abstract: Fibroblast growth factor receptors (FGFRs) have emerged as promising targets for anticancer therapy. In this study, we synthesized and evaluated the biological activity of 66 pyrazolo[3,4-