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Discovery of N-substituted 7-azaindoles as PIM1 kinase inhibitors - Part I.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2017 Oct 15; Vol. 27 (20), pp. 4730-4734. Date of Electronic Publication: 2017 Sep 18. - Publication Year :
- 2017
-
Abstract
- Novel N-substituted azaindoles have been discovered as PIM1 inhibitors. X-ray structures have played a significant role in orienting the chemistry effort in the initial phase of hit confirmation. Disclosure of an unconventional binding mode for 1 and 2, as demonstrated by X-ray crystallography, is presented and was an important factor in selecting and advancing a lead series.<br /> (Copyright © 2017 Elsevier Ltd. All rights reserved.)
- Subjects :
- Binding Sites
Cell Line, Tumor
Cell Proliferation drug effects
Crystallography, X-Ray
Drug Evaluation, Preclinical
Drug Screening Assays, Antitumor
Humans
Indoles metabolism
Inhibitory Concentration 50
Molecular Dynamics Simulation
Protein Kinase Inhibitors chemistry
Protein Serine-Threonine Kinases antagonists & inhibitors
Protein Serine-Threonine Kinases metabolism
Protein Structure, Tertiary
Proto-Oncogene Proteins antagonists & inhibitors
Proto-Oncogene Proteins metabolism
Proto-Oncogene Proteins c-pim-1 metabolism
Structure-Activity Relationship
Indoles chemistry
Indoles pharmacology
Protein Kinase Inhibitors metabolism
Protein Kinase Inhibitors pharmacology
Proto-Oncogene Proteins c-pim-1 antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 27
- Issue :
- 20
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 28947155
- Full Text :
- https://doi.org/10.1016/j.bmcl.2017.08.069