title: Identification of a pharmacophore for thrombopoietic activity of small, non-peptidyl molecules. 2. Rational design of naphtho[1,2-d]imidazole thrombopoietin mimics.
abstract: The invention of a new class of naphtho[1,2-d]imidazole thrombopoietin mimics based on a pharmacophore hypothesis for small-molecule thrombopoietic agonists is discussed. Parallel array synthesis and purification techniques allowed for the rapid exploration of structure-activity relationships within this class and for the improvement in TPO mimetic potencies and efficacies.
authors.forename: Kevin J
authors.initials: KJ
authors.lastname: Duffy
authors.forename: Alan T
authors.initials: AT
authors.lastname: Price
authors.forename: Evelyne
authors.initials: E
authors.lastname: Delorme
authors.forename: Susan B
authors.initials: SB
authors.lastname: Dillon
authors.forename: Celine
authors.initials: C
authors.lastname: Duquenne
authors.forename: Connie
authors.initials: C
authors.lastname: Erickson-Miller
authors.forename: Leslie
authors.initials: L
authors.lastname: Giampa
authors.forename: Yifang
authors.initials: Y
authors.lastname: Huang
authors.forename: Richard M
authors.initials: RM
authors.lastname: Keenan
authors.forename: Peter
authors.initials: P
authors.lastname: Lamb
authors.forename: Nannan
authors.initials: N
authors.lastname: Liu
authors.forename: Stephen G
authors.initials: SG
authors.lastname: Miller
authors.forename: Jon
authors.initials: J
authors.lastname: Rosen
authors.forename: Anthony N
authors.initials: AN
authors.lastname: Shaw
authors.forename: Heather
authors.initials: H
authors.lastname: Smith
authors.forename: Kenneth J
authors.initials: KJ
authors.lastname: Wiggall
authors.forename: Lihua
authors.initials: L
authors.lastname: Zhang
authors.forename: Juan I
authors.initials: JI
authors.lastname: Luengo
mesh_terms: D018952:Antigens, CD34 / Q000378:metabolism; D001854:Bone Marrow Cells / Q000187:drug effects / Q000378:metabolism; D002454:Cell Differentiation; D002455:Cell Division / Q000187:drug effects; D002460:Cell Line; D020650:Combinatorial Chemistry Techniques; D017930:Genes, Reporter; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008156:Luciferases / Q000235:genetics / Q000378:metabolism; D008958:Models, Molecular; D018716:Molecular Mimicry; D010766:Phosphorylation; D013329:Structure-Activity Relationship; D013926:Thrombopoietin / Q000737:chemistry* / Q000235:genetics / Q000494:pharmacology
chemical_list: D018952:Antigens, CD34; D007093:Imidazoles; D013926:Thrombopoietin; D008156:Luciferases