title: 4-Substituted quinazoline derivatives as novel EphA2 receptor tyrosine kinase inhibitors.
abstract: Erythropoietin-producing hepatocellular receptor tyrosine kinase subtype A2 (EphA2) is an attractive therapeutic target for suppressing tumor progression. In our efforts to discover novel small molecules to inhibit EphA2, a class of compound based on 4-substituted quinazoline containing 7-(morpholin-2-ylmethoxy) group was identified as a novel hit by high throughput screening campaign. Structural modification of parent quinazoline scaffolds by introducing substituents on aniline displayed potent inhibitory activities toward EphA2.
authors.affiliation: Research Center for Medicinal Chemistry, Korea Research Institute of Chemical Technology, Yuseong-gu, Daejeon 305-343, Republic of Korea.
authors.forename: Chae Jo
authors.initials: CJ
authors.lastname: Lim
authors.affiliation: Research Center for Drug Discovery Technology, Korea Research Institute of Chemical Technology, Yuseong-gu, Daejeon 305-343, Republic of Korea.
authors.forename: Kwang-Seok
authors.initials: KS
authors.lastname: Oh
authors.affiliation: Research Center for Medicinal Chemistry, Korea Research Institute of Chemical Technology, Yuseong-gu, Daejeon 305-343, Republic of Korea.
authors.forename: Jae Du
authors.initials: JD
authors.lastname: Ha
authors.affiliation: Research Center for Drug Discovery Technology, Korea Research Institute of Chemical Technology, Yuseong-gu, Daejeon 305-343, Republic of Korea.
authors.forename: Jeong Hyun
authors.initials: JH
authors.lastname: Lee
authors.affiliation: Research Center for Drug Discovery Technology, Korea Research Institute of Chemical Technology, Yuseong-gu, Daejeon 305-343, Republic of Korea.
authors.forename: Ho Won
authors.initials: HW
authors.lastname: Seo
authors.affiliation: Research Center for Drug Discovery Technology, Korea Research Institute of Chemical Technology, Yuseong-gu, Daejeon 305-343, Republic of Korea.
authors.forename: Chong Hack
authors.initials: CH
authors.lastname: Chae
authors.affiliation: Department of Internal Medicine, Chonbuk National University Medical School and Hospital, Jeonju 561-712, Republic of Korea.
authors.forename: Dae-Ghon
authors.initials: DG
authors.lastname: Kim
authors.affiliation: Department of Internal Medicine, Chonbuk National University Medical School and Hospital, Jeonju 561-712, Republic of Korea.
authors.forename: Mi-Jin
authors.initials: MJ
authors.lastname: Lee
authors.affiliation: Research Center for Drug Discovery Technology, Korea Research Institute of Chemical Technology, Yuseong-gu, Daejeon 305-343, Republic of Korea. Electronic address: bhlee@krict.re.kr.
authors.forename: Byung Ho
authors.initials: BH
authors.lastname: Lee
mesh_terms: D004305:Dose-Response Relationship, Drug; D006801:Humans; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011799:Quinazolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D036104:Receptor, EphA2 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D036104:Receptor, EphA2
keywords: Breast cancer; Epithelial cell kinase (Eck); Erythropoietin-producing hepatocellular receptor tyrosine kinase subtype A2 (EphA2); Quinazoline