Amidine analogues of melphalan: synthesis, cytotoxic activity, and DNA binding properties
| Autor: | Tomasz Anchim, Krzysztof Bielawski, Anna Bielawska |
|---|---|
| Rok vydání: | 2007 |
| Předmět: |
Melphalan
Cell Survival Amidines Pharmaceutical Science Antineoplastic Agents Breast Neoplasms Amidine chemistry.chemical_compound Inhibitory Concentration 50 Structure-Activity Relationship hemic and lymphatic diseases Cell Line Tumor Ethidium Drug Discovery medicine Cytotoxic T cell Humans Topoisomerase II Inhibitors MTT assay Cytotoxicity Cell Proliferation biology Topoisomerase General Medicine DNA chemistry Biochemistry Cancer cell biology.protein Drug Screening Assays Antitumor Topoisomerase I Inhibitors medicine.drug Thymidine |
| Zdroj: | Archiv der Pharmazie. 340(5) |
| ISSN: | 0365-6233 |
| Popis: | Design, synthesis, and cytotoxic activity of amidine derivatives of melphalan are described and structure-activity relationships are discussed. Evaluation of the cytotoxicity of these compounds employing a MTT assay and inhibition of [(3)H]thymidine incorporation into DNA in both MDA-MB-231 and MCF-7 human breast cancer cells demonstrated that these compounds were more active than melphalan. Data from the ethidium displacement assay showed that these compounds were able to bind in the minor groove-binding mode in AT sequences of DNA. The cytotoxic properties of the amidine analogues of melphalan towards cultured human breast cancer cells correlate with topoisomerase II inhibitory properties but not with DNA-binding properties. |
| Databáze: | OpenAIRE |
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