Structure-activity relationship studies of flavopiridol analogues.
Cyclin dependent kinases (CDKs) along with the complementary cyclins form key regulatory checkpoint controls on the cell cycle. Flavopiridol is a synthetic flavone that shows potent and selective cyclin-dependent kinase inhibitory activity. In this paper, we report modifications of the 3-hydroxy-1-methylpiperidinyl (D ring) of flavopiridol and their effect on CDK inhibitory activity.
Murthi
K K
KK
Department of Medicinal Chemistry, Mitotix Inc., Cambridge, MA 02139, USA. murthi@mitotix.com
Dubay
M
M
McClure
C
C
Brizuela
L
L
Boisclair
M D
MD
Worland
P J
PJ
Mansuri
M M
MM
Pal
K
K
D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D002867:Chromones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D005419:Flavonoids / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D010880:Piperidines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
C413727:2-(2-chlorophenyl)-5,7-dihydroxy-8-(2,3,6-trihydro-1-methylpyridin-4-yl)benzopyran-4-one; D000970:Antineoplastic Agents; D002867:Chromones; D004791:Enzyme Inhibitors; D005419:Flavonoids; D010880:Piperidines; D011725:Pyridines; C077990:alvocidib; D018844:Cyclin-Dependent Kinases