title: Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1.
abstract: A series of 2-amino-9-aryl-7H-pyrrolo[2,3-d]pyrimidines were designed and synthesized to target focal adhesion kinase (FAK). A number of these pyrrolopyrimides exhibited low micromolar inhibitory activities against focal adhesion kinase, and their preliminary SAR was established via systematic chemical modifications. The 2-amino-9-aryl-7H-pyrrolo[2,3-d]pyrimidines represent a new class of kinase inhibitors.
authors.affiliation: Genomics Institute of the Novartis Research Foundation (GNF), 10715 John Jay Hopkins Drive, San Diego, CA 920121, USA.
authors.forename: Ha-Soon
authors.initials: HS
authors.lastname: Choi
authors.forename: Zhicheng
authors.initials: Z
authors.lastname: Wang
authors.forename: Wendy
authors.initials: W
authors.lastname: Richmond
authors.forename: Xiaohui
authors.initials: X
authors.lastname: He
authors.forename: Kunyong
authors.initials: K
authors.lastname: Yang
authors.forename: Tao
authors.initials: T
authors.lastname: Jiang
authors.forename: Taebo
authors.initials: T
authors.lastname: Sim
authors.forename: Donald
authors.initials: D
authors.lastname: Karanewsky
authors.forename: Xiang-ju
authors.initials: XJ
authors.lastname: Gu
authors.forename: Vicki
authors.initials: V
authors.lastname: Zhou
authors.forename: Yi
authors.initials: Y
authors.lastname: Liu
authors.forename: Osamu
authors.initials: O
authors.lastname: Ohmori
authors.forename: Jeremy
authors.initials: J
authors.lastname: Caldwell
authors.forename: Nathanael
authors.initials: N
authors.lastname: Gray
authors.forename: Yun
authors.initials: Y
authors.lastname: He
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D051416:Focal Adhesion Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D006801:Humans; D011743:Pyrimidines / Q000138:chemical synthesis / Q000494:pharmacology; D011758:Pyrroles / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011743:Pyrimidines; D011758:Pyrroles; D051416:Focal Adhesion Protein-Tyrosine Kinases