title: Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors.
abstract: The synthesis of novel aza-1,7-annulated indoles was achieved and these were converted to indolocarbazoles that proved to be potent kinase inhibitors. These compounds were also evaluated in a human colon carcinoma cell line and proved to be good antiproliferative agents.
authors.affiliation: Discovery Chemistry Research, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA. al-awar_rima_s@lilly.com
authors.forename: Rima S
authors.initials: RS
authors.lastname: Al-awar
authors.forename: James E
authors.initials: JE
authors.lastname: Ray
authors.forename: Kyle A
authors.initials: KA
authors.lastname: Hecker
authors.forename: Sajan
authors.initials: S
authors.lastname: Joseph
authors.forename: Jianping
authors.initials: J
authors.lastname: Huang
authors.forename: Chuan
authors.initials: C
authors.lastname: Shih
authors.forename: Harold B
authors.initials: HB
authors.lastname: Brooks
authors.forename: Charles D
authors.initials: CD
authors.lastname: Spencer
authors.forename: Scott A
authors.initials: SA
authors.lastname: Watkins
authors.forename: Richard M
authors.initials: RM
authors.lastname: Schultz
authors.forename: Eileen L
authors.initials: EL
authors.lastname: Considine
authors.forename: Margaret M
authors.initials: MM
authors.lastname: Faul
authors.forename: Kevin A
authors.initials: KA
authors.lastname: Sullivan
authors.forename: Stanley P
authors.initials: SP
authors.lastname: Kolis
authors.forename: Michael A
authors.initials: MA
authors.lastname: Carr
authors.forename: Faming
authors.initials: F
authors.lastname: Zhang
mesh_terms: D001372:Aza Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D001665:Binding Sites; D042846:CDC2-CDC28 Kinases / Q000037:antagonists & inhibitors* / Q000737:chemistry; D002453:Cell Cycle / Q000187:drug effects; D051357:Cyclin-Dependent Kinase 2; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008958:Models, Molecular; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D001372:Aza Compounds; D004791:Enzyme Inhibitors; D007211:Indoles; D042846:CDC2-CDC28 Kinases; D051357:Cyclin-Dependent Kinase 2