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Synthesis and in vitro growth inhibitory activity of novel silyl- and trityl-modified nucleosides
- Source :
- Bioorganic & Medicinal Chemistry. 24:2716-2724
- Publication Year :
- 2016
- Publisher :
- Elsevier BV, 2016.
-
Abstract
- Seventeen silyl- and trityl-modified (5′-O- and 3′,5′-di-O-) nucleosides were synthesized with the aim of investigating the in vitro antiproliferative activities of these nucleoside derivatives. A subset of the compounds was evaluated at a fixed concentration of 100 μM against a small panel of tumor cell lines (HL-60, K-562, Jurkat, Caco-2 and HT-29). The entire set was also tested at varying concentrations against two human glioma lines (U373 and Hs683) to obtain GI50 values, with the best results being values of ∼25 μM.
- Subjects :
- Silylation
Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Antineoplastic Agents
010402 general chemistry
Inhibitory postsynaptic potential
01 natural sciences
Biochemistry
Jurkat cells
Structure-Activity Relationship
Cell Line, Tumor
Neoplasms
Drug Discovery
Humans
Structure–activity relationship
Molecular Biology
Cell Proliferation
010405 organic chemistry
Chemistry
Cell growth
Organic Chemistry
Nucleosides
In vitro
0104 chemical sciences
Molecular Medicine
In vitro growth
Nucleoside
Subjects
Details
- ISSN :
- 09680896
- Volume :
- 24
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry
- Accession number :
- edsair.doi.dedup.....355f2e6e566c92218a54fe9ef830f9f0