Synthesis and characterization of novel 1,2,4-triazine derivatives with antiproliferative activity
| Autor: | Hans-Hermann Rüttinger, P. Frohberg, Hans-Martin Dahse, Fabian Krauth |
|---|---|
| Rok vydání: | 2010 |
| Předmět: |
Human leukemia
Pyrrolidines Stereochemistry Clinical Biochemistry Serum albumin Pharmaceutical Science Antineoplastic Agents Biochemistry Cell Line Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Humans Cytotoxicity Molecular Biology Serum Albumin Triazine biology Triazines Organic Chemistry Small molecule In vitro chemistry Cell culture Lipinski's rule of five biology.protein Molecular Medicine K562 Cells HeLa Cells Protein Binding |
| Zdroj: | Bioorganic & Medicinal Chemistry. 18:1816-1821 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2010.01.053 |
| Popis: | A series of novel small molecules with a 1,2,4-triazine scaffold was obtained according to a recently published and highly efficient synthetic route. Screening for antiproliferative and cytotoxic activity revealed distinct anticancer effects against the human leukemia cell line K-562 combined with a remarkable low cytotoxicity. All compounds were in agreement with the ‘rule-of-five’ claims by Lipinski and calculated log Pcalc values were experimentally confirmed (log Pexp). For the most active compounds, in vitro serum albumin binding was investigated and structure–activity relationships were established. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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