Synthesis and in vitro growth inhibitory activity of novel silyl- and trityl-modified nucleosides
| Autor: | Ivan R. Green, Willem A. L. van Otterlo, M.E. Christine Rey, Stephen C. Pelly, Laetitia Moreno Y Banuls, Leonie Harmse, Helen Apostolellis, Alexander Kornienko, Nurit Dahan-Farkas, Robert Kiss, Hajierah Davids, Jenny-Lee Panayides, Véronique Mathieu |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
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 |
| Zdroj: | Bioorganic & Medicinal Chemistry. 24:2716-2724 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2016.04.036 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect