Synthesis and biological activity of olomoucine II
Language English Country England, Great Britain Media print
Document type Comparative Study, Journal Article, Research Support, Non-U.S. Gov't
PubMed
12392733
DOI
10.1016/s0960-894x(02)00693-5
PII: S0960894X02006935
Knihovny.cz E-resources
- MeSH
- Antineoplastic Agents chemical synthesis pharmacology MeSH
- Enzyme Inhibitors chemical synthesis pharmacology MeSH
- Kinetin MeSH
- Drug Screening Assays, Antitumor MeSH
- Humans MeSH
- Tumor Cells, Cultured MeSH
- CDC2 Protein Kinase antagonists & inhibitors MeSH
- CDC28 Protein Kinase, S cerevisiae antagonists & inhibitors MeSH
- Purines chemical synthesis pharmacology MeSH
- Roscovitine MeSH
- Cell Survival drug effects MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Comparative Study MeSH
- Names of Substances
- 6-((3-chloro)anilino)-2-(isopropyl-2-hydroxyethylamino)-9-isopropylpurine MeSH Browser
- Antineoplastic Agents MeSH
- Enzyme Inhibitors MeSH
- Kinetin MeSH
- olomoucine II MeSH Browser
- olomoucine MeSH Browser
- CDC2 Protein Kinase MeSH
- CDC28 Protein Kinase, S cerevisiae MeSH
- Purines MeSH
- Roscovitine MeSH
Based on our previous experiences with synthesis of purines, novel 2,6,9-trisubstituted purine derivatives were prepared and assayed for the ability to inhibit CDK1/cyclin B kinase. One of newly synthesized compounds designated as olomoucine II, 6-[(2-hydroxybenzyl)amino]-2-[[1-(hydroxymethyl)propyl]amino]-9-isopropylpurine, displays 10 times higher inhibitory activity than roscovitine, potent and specific CDK1 inhibitor. Olomoucine II in vitro cytotoxic activity exceeds purvalanol A, the most potent CDK inhibitor, as it kills the CEM cells with IC(50) value of 3.0 microM.
References provided by Crossref.org
Adamantane-Substituted Purines and Their β-Cyclodextrin Complexes: Synthesis and Biological Activity
The inhibitor of cyclin-dependent kinases, olomoucine II, exhibits potent antiviral properties
