title: Acryloylamino-salicylanilides as EGFR PTK inhibitors.
abstract: A series of acryloylamino-salicylanilides were synthesized as inhibitors of EGFR PTK. A strategy of pseudo six-membered ring formed through intramolecular hydrogen bonding in salicylanilides is employed to mimic the planar pyrimidine ring of quinazoline EGFR inhibitors. Acrylamido moiety is incorporated to target the Cys-773 of EGFR specifically. Some of the obtained compounds exhibited good activity as EGFR inhibitors.
authors.affiliation: Department of Synthetic Medicinal Chemistry, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, PR China.
authors.forename: Wei
authors.initials: W
authors.lastname: Deng
authors.forename: Zongru
authors.initials: Z
authors.lastname: Guo
authors.forename: Yanshen
authors.initials: Y
authors.lastname: Guo
authors.forename: Zhiqiang
authors.initials: Z
authors.lastname: Feng
authors.forename: Yi
authors.initials: Y
authors.lastname: Jiang
authors.forename: Fengming
authors.initials: F
authors.lastname: Chu
mesh_terms: D018360:Crystallography, X-Ray; D015195:Drug Design; D066246:ErbB Receptors / Q000037:antagonists & inhibitors*; D008958:Models, Molecular; D015394:Molecular Structure; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D012458:Salicylanilides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D012458:Salicylanilides; D066246:ErbB Receptors; D011505:Protein-Tyrosine Kinases