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Structure-based design and SAR development of 5,6-dihydroimidazolo[1,5-f]pteridine derivatives as novel Polo-like kinase-1 inhibitors.
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Mar2017, Vol. 27 Issue 5, p1311-1315. 5p. - Publication Year :
- 2017
-
Abstract
- Using structure-based drug design, we identified a novel series of 5,6-dihydroimidazolo[1,5- f ]pteridine PLK1 inhibitors. Rational improvements to compounds of this class resulted in single-digit nanomolar enzyme and cellular activity against PLK1, and oral bioavailability. Compound 1 exhibits >7 fold induction of phosphorylated Histone H3 and is efficacious in an in vivo HT-29 tumor xenograft model. [ABSTRACT FROM AUTHOR]
- Subjects :
- *DRUG design
*ENZYME inhibitors
*BIOAVAILABILITY
*PHOSPHORYLATION
*XENOGRAFTS
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 27
- Issue :
- 5
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 121358781
- Full Text :
- https://doi.org/10.1016/j.bmcl.2016.10.009