Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors

Shudong Wang; Gavin Wood; Christopher Meades; Gary Griffiths; Carol Midgley; Iain McNae; Campbell McInnes; Sian Anderson; Wayne Jackson; Mokdad Mezna; Rhoda Yuill; Malcolm Walkinshaw; Peter M Fischer

doi:10.1016/j.bmcl.2004.06.012

Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors

Bioorg Med Chem Lett. 2004 Aug 16;14(16):4237-40. doi: 10.1016/j.bmcl.2004.06.012.

Authors

Shudong Wang¹, Gavin Wood, Christopher Meades, Gary Griffiths, Carol Midgley, Iain McNae, Campbell McInnes, Sian Anderson, Wayne Jackson, Mokdad Mezna, Rhoda Yuill, Malcolm Walkinshaw, Peter M Fischer

Affiliation

¹ Cyclacel Limited, James Lindsay Place, Dundee DD1 5JJ, Scotland, UK. swang@cyclacel.com

PMID: 15261277
DOI: 10.1016/j.bmcl.2004.06.012

Abstract

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.

MeSH terms

Cell Line, Tumor
Cyclin-Dependent Kinases / antagonists & inhibitors*
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Humans
Models, Molecular
Pyrimidines / chemical synthesis*
Pyrimidines / chemistry
Pyrimidines / pharmacology
Pyrroles / chemical synthesis*
Pyrroles / chemistry
Pyrroles / pharmacology
Structure-Activity Relationship

Substances

2-anilino-4-(1H-pyrrol-3-yl) pyrimidine
Enzyme Inhibitors
Pyrimidines
Pyrroles
Cyclin-Dependent Kinases