A Novel Pyrazolo[1,5-a]pyrimidine Is a Potent Inhibitor of Cyclin-Dependent Protein Kinases 1, 2, and 9, Which Demonstrates Antitumor Effects in Human Tumor Xenografts Following Oral Administration

Heathcote DA, Patel H, Kroll SHB, Hazel P, Periyasamy M, Alikian M, Kanneganti SK, Jogalekar AS, Scheiper B, Barbazanges M, Blum A, Brackow J

et al

23 December 2010

Journal article

Journal:

Journal of Medicinal Chemistry

Volume:

Issue:

American Chemical Society (ACS)

pp.

8508 - 8522

No abstract available

Keywords:

32 Biomedical and Clinical Sciences

3211 Oncology and Carcinogenesis

Biotechnology

Rare Diseases

Cancer

5.1 Pharmaceuticals

Cancer

Administration, Oral

Animals

Antineoplastic Agents

Biological Availability

Blood Proteins

Cell Cycle

Cell Line, Tumor

Cell Proliferation

Crystallography, X-Ray

Cyclin-Dependent Kinase 2

Cyclin-Dependent Kinase 9

Female

Humans

In Vitro Techniques

Mice

Mice, Nude

Microsomes, Liver

Models, Molecular

Phosphorylation

Protein Binding

Pyrazoles

Pyrimidines

Stereoisomerism

Structure-Activity Relationship

Xenograft Model Antitumor Assays

DOI