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Identification of 1,6-dihydropyrazolo[4,3-c]carbazoles and 3,6-dihydropyrazolo[3,4-c]carbazoles as new Pim kinase inhibitors.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2013 Jul 15; Vol. 21 (14), pp. 4102-11. Date of Electronic Publication: 2013 May 16. - Publication Year :
- 2013
-
Abstract
- New 1,6-dihydropyrazolo[4,3-c]carbazoles and 3,6-dihydropyrazolo[3,4-c]carbazoles were prepared and evaluated for their Pim kinase inhibitory potencies as well as their antiproliferative activities toward two prostatic cancer cell lines. Pyrazolocarbazole 15a was found to be a potent Pim kinase modulator with inhibitory potency toward the three isoforms. Compound 6c strongly inhibited Pim-3 with weaker effect toward Pim-1 and Pim-2, and thus could be used as an interesting molecular tool to study Pim-3 biological functions.<br /> (Copyright © 2013 Elsevier Ltd. All rights reserved.)
- Subjects :
- Carbazoles chemical synthesis
Carbazoles pharmacology
Cell Line, Tumor
Cell Proliferation drug effects
Humans
Inhibitory Concentration 50
Male
Models, Molecular
Prostatic Neoplasms drug therapy
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors chemistry
Pyrazoles chemical synthesis
Pyrazoles chemistry
Pyrazoles pharmacology
Carbazoles chemistry
Protein Kinase Inhibitors pharmacology
Proto-Oncogene Proteins c-pim-1 antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 21
- Issue :
- 14
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 23735828
- Full Text :
- https://doi.org/10.1016/j.bmc.2013.05.011