Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors.
A series of 2-anilino-4-(1H-pyrrol-3-yl)pyrimidines were prepared and evaluated for their ability to inhibit cyclin-dependent kinases (CDKs). A number of analogues were found to be potent CDK2 and CDK4 inhibitors and to exhibit anti-proliferative activity against human tumour cell lines. Structure-activity relationships and biochemical characterization are presented.
Wang
Shudong
S
Cyclacel Limited, James Lindsay Place, Dundee DD1 5JJ, Scotland, UK. swang@cyclacel.com
Wood
Gavin
G
Meades
Christopher
C
Griffiths
Gary
G
Midgley
Carol
C
McNae
Iain
I
McInnes
Campbell
C
Anderson
Sian
S
Jackson
Wayne
W
Mezna
Mokdad
M
Yuill
Rhoda
R
Walkinshaw
Malcolm
M
Fischer
Peter M
PM
D045744:Cell Line, Tumor; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008958:Models, Molecular; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011758:Pyrroles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
C496609:2-anilino-4-(1H-pyrrol-3-yl) pyrimidine; D004791:Enzyme Inhibitors; D011743:Pyrimidines; D011758:Pyrroles; D018844:Cyclin-Dependent Kinases