title: Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization.
abstract: Based on an (aminoaryl)benzothiazole quinazoline hit structure for kinase inhibition, a systematic optimization program resulted in a lead structure allowing for inhibitory activities in cellular phosphorylation assays in the low nanomolar range.
authors.affiliation: 4SC AG, Am Klopferspitz 19a, 82152 Planegg-Martinsried, Germany.
authors.forename: Stefan
authors.initials: S
authors.lastname: Tasler
authors.forename: Oliver
authors.initials: O
authors.lastname: Müller
authors.forename: Tanja
authors.initials: T
authors.lastname: Wieber
authors.forename: Thomas
authors.initials: T
authors.lastname: Herz
authors.forename: Stefano
authors.initials: S
authors.lastname: Pegoraro
authors.forename: Wael
authors.initials: W
authors.lastname: Saeb
authors.forename: Martin
authors.initials: M
authors.lastname: Lang
authors.forename: Rolf
authors.initials: R
authors.lastname: Krauss
authors.forename: Frank
authors.initials: F
authors.lastname: Totzke
authors.forename: Ute
authors.initials: U
authors.lastname: Zirrgiebel
authors.forename: Jan E
authors.initials: JE
authors.lastname: Ehlert
authors.forename: Michael H G
authors.initials: MH
authors.lastname: Kubbutat
authors.forename: Christoph
authors.initials: C
authors.lastname: Schächtele
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D064127:Aurora Kinases; D052160:Benzothiazoles / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D066246:ErbB Receptors / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D010766:Phosphorylation / Q000187:drug effects; D011485:Protein Binding; D047428:Protein Kinase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D011494:Protein Kinases / Q000737:chemistry / Q000378:metabolism*; D017346:Protein Serine-Threonine Kinases / Q000737:chemistry / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D052160:Benzothiazoles; D047428:Protein Kinase Inhibitors; D011494:Protein Kinases; D066246:ErbB Receptors; D064127:Aurora Kinases; D017346:Protein Serine-Threonine Kinases; C005465:benzothiazole