Molecular design and synthesis of new heterobivalent compounds based on chlorambucil and colchicine
| Autor: | Nele Fritsch, Elena R. Milaeva, N. A. Zefirov, Sergei A. Kuznetsov, Evgenia V. Nurieva, Olga N. Zefirova |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Chlorambucil
biology 010405 organic chemistry Chemistry General Chemistry 010402 general chemistry 01 natural sciences Combinatorial chemistry 0104 chemical sciences chemistry.chemical_compound Tubulin Microtubule Depolymerization medicine biology.protein Colchicine Molecule Selectivity medicine.drug Conjugate |
| Zdroj: | Mendeleev Communications. 30:706-708 |
| ISSN: | 0959-9436 |
| DOI: | 10.1016/j.mencom.2020.11.005 |
| Popis: | Two new heterobivalent molecules were designed by linking a DNA-alkylating agent chlorambucil with tubulin-targeting compound colchicine or its adamantyl containing C(7)-derivative. Target compounds were synthesized via acid coupling with N-deacetylcolchicine. According to preliminary biotests, both conjugates caused microtubule depolymerization and strong tubulin clustering, and colchicine–chlorambucil conjugate was found to be one order of magnitude more potent and to exhibit some selectivity to A549 carcinoma cells. |
| Databáze: | OpenAIRE |
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