title: Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.
abstract: We report the discovery and preliminary SAR studies of a series of structurally novel benzotriazine core based small molecules as inhibitors of Src kinase. To the best of our knowledge, benzotriazine template based compounds have not been reported as kinase inhibitors. The 3-(2-(1-pyrrolidinyl)ethoxy)phenyl analogue (43) was identified as one of the most potent inhibitors of Src kinase.
authors.affiliation: TargeGen, Inc., 9380 Judicial Drive, San Diego, CA 92121, USA. noronha@targegen.com
authors.forename: Glenn
authors.initials: G
authors.lastname: Noronha
authors.forename: Kathy
authors.initials: K
authors.lastname: Barrett
authors.forename: Jianguo
authors.initials: J
authors.lastname: Cao
authors.forename: Elena
authors.initials: E
authors.lastname: Dneprovskaia
authors.forename: Richard
authors.initials: R
authors.lastname: Fine
authors.forename: Xianchang
authors.initials: X
authors.lastname: Gong
authors.forename: Colleen
authors.initials: C
authors.lastname: Gritzen
authors.forename: John
authors.initials: J
authors.lastname: Hood
authors.forename: Xinshan
authors.initials: X
authors.lastname: Kang
authors.forename: Boris
authors.initials: B
authors.lastname: Klebansky
authors.forename: G
authors.initials: G
authors.lastname: Li
authors.forename: W
authors.initials: W
authors.lastname: Liao
authors.forename: Dan
authors.initials: D
authors.lastname: Lohse
authors.forename: Chi Ching
authors.initials: CC
authors.lastname: Mak
authors.forename: Andrew
authors.initials: A
authors.lastname: McPherson
authors.forename: Moorthy S S
authors.initials: MS
authors.lastname: Palanki
authors.forename: Ved P
authors.initials: VP
authors.lastname: Pathak
authors.forename: Joel
authors.initials: J
authors.lastname: Renick
authors.forename: Richard
authors.initials: R
authors.lastname: Soll
authors.forename: Ute
authors.initials: U
authors.lastname: Splittgerber
authors.forename: Wolfgang
authors.initials: W
authors.lastname: Wrasidlo
authors.forename: Binqi
authors.initials: B
authors.lastname: Zeng
authors.forename: Ningning
authors.initials: N
authors.lastname: Zhao
authors.forename: Y
authors.initials: Y
authors.lastname: Zhou
mesh_terms: D006801:Humans; D016392:Proto-Oncogene Proteins pp60(c-src) / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014227:Triazines / Q000494:pharmacology*
chemical_list: D014227:Triazines; D016392:Proto-Oncogene Proteins pp60(c-src)