title: Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors.
abstract: A series of novel pyrrolopyridazine derivatives have been discovered to be HER-2 inhibitors. These compounds selectively inhibited HER-2 kinase activity at low nanomolar concentrations. Compound 7d was identified as a potent HER-2 inhibitor with an IC(50) of 4 nM.
authors.affiliation: Shanghai Hengrui Pharmaceuticals Co., Ltd., 279 Wenjing Road, Shanghai 200245, China. tangpc@shhrp.com
authors.forename: Peng Cho
authors.initials: PC
authors.lastname: Tang
authors.forename: Jun
authors.initials: J
authors.lastname: Feng
authors.forename: Li
authors.initials: L
authors.lastname: Huang
authors.forename: Zhe
authors.initials: Z
authors.lastname: Xu
authors.forename: Ling
authors.initials: L
authors.lastname: Cheng
authors.forename: Xu
authors.initials: X
authors.lastname: Zhang
authors.forename: Lei
authors.initials: L
authors.lastname: Zhang
authors.forename: Bing
authors.initials: B
authors.lastname: Hu
mesh_terms: D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D008958:Models, Molecular; D011724:Pyridazines / Q000138:chemical synthesis / Q000494:pharmacology*; D011758:Pyrroles / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D053634:TYK2 Kinase / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D011724:Pyridazines; D011758:Pyrroles; C508945:Pyrrolopyridazine; D053634:TYK2 Kinase