Please use this identifier to cite or link to this item:
https://hdl.handle.net/2440/127114
Citations | ||
Scopus | Web of Science® | Altmetric |
---|---|---|
?
|
?
|
Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Tadesse, S. | - |
dc.contributor.author | Zhu, G. | - |
dc.contributor.author | Mekonnen, L.B. | - |
dc.contributor.author | Lenjisa, J.L. | - |
dc.contributor.author | Yu, M. | - |
dc.contributor.author | Brown, M.P. | - |
dc.contributor.author | Wang, S. | - |
dc.date.issued | 2017 | - |
dc.identifier.citation | Future Medicinal Chemistry, 2017; 9(13):1495-1506 | - |
dc.identifier.issn | 1756-8919 | - |
dc.identifier.issn | 1756-8927 | - |
dc.identifier.uri | http://hdl.handle.net/2440/127114 | - |
dc.description.abstract | Inhibitors of CDK4/6 have emerged as a powerful class of therapeutics for treatment of several malignancies. We herein describe the identification of a new series of molecules that demonstrated excellent selectivity for CDK4/6 over CDKs1, 7 and 9.Medicinal chemistry optimization led to the discovery of 58 and 69 that inhibited CDK4 and CDK4/6, respectively, with high potency and selectivity, and 58 and 69 exhibited potent antiproliferative activities in a panel of human cancer cell lines including leukemia, and cancers of the breast, colon, ovary, pancreas and prostate.Compounds 58 and 69 caused remarkable growth inhibition of melanoma cells, particularly the cells harboring multiple BRAF and NRAS mutations, via a CDK4/6-targeted mechanism of action. [Formula: see text]. | - |
dc.description.statementofresponsibility | Solomon Tadesse, Ge Zhu, Laychiluh B Mekonnen, Jimma L Lenjisa, Mingfeng Yu, Michael P Brown, Shudong Wang | - |
dc.language.iso | en | - |
dc.publisher | Future Science | - |
dc.rights | © 2017 Future Science Ltd. | - |
dc.source.uri | http://dx.doi.org/10.4155/fmc-2017-0076 | - |
dc.subject | Cell Line, Tumor | - |
dc.subject | Humans | - |
dc.subject | Amines | - |
dc.subject | Pyridines | - |
dc.subject | Pyrimidines | - |
dc.subject | Thiazoles | - |
dc.subject | GTP Phosphohydrolases | - |
dc.subject | Proto-Oncogene Proteins B-raf | - |
dc.subject | Retinoblastoma Protein | - |
dc.subject | Membrane Proteins | - |
dc.subject | Protein Kinase Inhibitors | - |
dc.subject | Cell Proliferation | - |
dc.subject | Binding Sites | - |
dc.subject | Protein Structure, Tertiary | - |
dc.subject | Protein Binding | - |
dc.subject | Structure-Activity Relationship | - |
dc.subject | Phosphorylation | - |
dc.subject | Cyclin-Dependent Kinase 4 | - |
dc.subject | Cyclin-Dependent Kinase 6 | - |
dc.subject | G1 Phase Cell Cycle Checkpoints | - |
dc.title | A novel series of N-(pyridin-2-yl)-4-(thiazol-5-yl)pyrimidin-2-amines as highly potent CDK4/6 inhibitors | - |
dc.type | Journal article | - |
dc.identifier.doi | 10.4155/fmc-2017-0076 | - |
pubs.publication-status | Published | - |
dc.identifier.orcid | Brown, M.P. [0000-0002-5796-1932] [0000-0002-6678-1407] | - |
Appears in Collections: | Aurora harvest 4 Biochemistry publications |
Files in This Item:
There are no files associated with this item.
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.