Synthesis of 1,7-annulated indoles and their applications in the studies of cyclin dependent kinase inhibitors.
The synthesis of a novel series of 1,7-annulated indolocarbazoles 2 and 16 is described. These compounds were found to be potent cyclin dependent kinase inhibitors with good antiproliferative activity against two human carcinoma cell lines. These inhibitors also arrested tumor cells at the G1 phase and inhibited pRb phosphorylation.
Zhu
Guoxin
G
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA. zhu_guoxin@lilly.com
Conner
Scott E
SE
Zhou
Xun
X
Chan
Ho-Kit
HK
Shih
Chuan
C
Engler
Thomas A
TA
Al-Awar
Rima S
RS
Brooks
Harold B
HB
Watkins
Scott A
SA
Spencer
Charles D
CD
Schultz
Richard M
RM
Dempsey
Jack A
JA
Considine
Eileen L
EL
Patel
Bharvin R
BR
Ogg
Catherine A
CA
Vasudevan
Vasu
V
Lytle
Michelle L
ML
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D045744:Cell Line, Tumor; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006131:Growth Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology
D000970:Antineoplastic Agents; D006131:Growth Inhibitors; D007211:Indoles; D047428:Protein Kinase Inhibitors; D018844:Cyclin-Dependent Kinases