| Autor: |
Nalin, Seixas, Bruno B, Ravanello, Ibrahim, Morgan, Goran N, Kaluđerović, Ludger A, Wessjohann |
| Rok vydání: |
2018 |
| Předmět: |
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| Zdroj: |
Pharmaceutics |
| ISSN: |
1999-4923 |
| Popis: |
Herein, a new Ugi multicomponent reaction strategy is described to enhance activity and solubility of the chemotherapeutic drug chlorambucil through its conjugation to poly(amidoamine) (PAMAM-NH2) dendrimers with the simultaneous introduction of lipidic (i-Pr) and cationic (–NH2) or anionic (–COOH) groups. Standard viability assays were used to evaluate the anticancer potential of the water-soluble dendrimers against PC-3 prostate and HT-29 colon cancer cell lines, as well as non-cancerous mouse NIH3T3 fibroblasts. It could be demonstrated that the anticancer activity against PC-3 cells was considerably improved when both chlorambucil and –NH2 (cationic) groups were present on the dendrimer surface (1b). Additionally, this dendrimer showed activity only against the prostate cancer cells (PC-3), while it did not affect colon cancer cells and fibroblasts significantly. The cationic chlorambucil-dendrimer 1b blocks PC-3 cells in the G2/M phase and induces caspase independent apoptosis. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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