Synthesis, cytotoxic effects and tubulin polymerization inhibition of 1,4-disubstituted 1,2,3-triazole analogs of 2-methoxyestradiol.
Thirteen 1,4-disubstituted 1,2,3-triazole analogs of 2-methoxyestradiol were prepared and tested for their cytotoxic and tubulin polymerization inhibition effects. Two compounds, 11j and 11k, exhibited anti-proliferative effects at low micromolar concentrations. The two analogs 11j and 11k also inhibited tubulin assembly with IC50 values of 8.1 and 5.9μM, respectively.
['Solum|Eirik Johansson|EJ|', 'Vik|Anders|A|', 'Hansen|Trond Vidar|TV|']
D000077584:2-Methoxyestradiol D000970:Antineoplastic Agents D060326:Chemistry Techniques, Synthetic D004958:Estradiol D006801:Humans D020014:K562 Cells D055503:Protein Multimerization D020836:Protein Structure, Quaternary D014230:Triazoles D014404:Tubulin D050257:Tubulin Modulators
Cytotoxicity 1,2,3-Triazoles 2-Methoxyestradiol Anti-cancer Estrogens Tubulin inhibition