Preparation of novel aza-1,7-annulated indoles and their conversion to potent indolocarbazole kinase inhibitors.
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.
Al-awar
Rima S
RS
Discovery Chemistry Research, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA. al-awar_rima_s@lilly.com
Ray
James E
JE
Hecker
Kyle A
KA
Joseph
Sajan
S
Huang
Jianping
J
Shih
Chuan
C
Brooks
Harold B
HB
Spencer
Charles D
CD
Watkins
Scott A
SA
Schultz
Richard M
RM
Considine
Eileen L
EL
Faul
Margaret M
MM
Sullivan
Kevin A
KA
Kolis
Stanley P
SP
Carr
Michael A
MA
Zhang
Faming
F
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
D001372:Aza Compounds; D004791:Enzyme Inhibitors; D007211:Indoles; D042846:CDC2-CDC28 Kinases; D051357:Cyclin-Dependent Kinase 2