Synthesis and biological evaluations of new analogs of 2-methoxyestradiol: Inhibitors of tubulin and angiogenesis
EJ Solum, JJ Cheng, IB Sørvik, RE Paulsen… - European Journal of …, 2014 - Elsevier
European Journal of Medicinal Chemistry, 2014•Elsevier
The synthesis, cytotoxicity, inhibition of tubulin polymerization and anti-angiogenic effects of
15 analogs of 2-methoxyestradiol (1) are reported. The biological studies revealed that the
position of nitrogen atom in the heterocyclic ring is important for inhibition of both tubulin
polymerization and angiogenesis. The most potent inhibitors were compounds 11f and 13e,
with a 6-substituted isoquinoline ring in the 17-position of the steroid skeleton. Moreover,
low estrogen activity was observed for the analogs tested at 10 μM concentrations.
15 analogs of 2-methoxyestradiol (1) are reported. The biological studies revealed that the
position of nitrogen atom in the heterocyclic ring is important for inhibition of both tubulin
polymerization and angiogenesis. The most potent inhibitors were compounds 11f and 13e,
with a 6-substituted isoquinoline ring in the 17-position of the steroid skeleton. Moreover,
low estrogen activity was observed for the analogs tested at 10 μM concentrations.
Abstract
The synthesis, cytotoxicity, inhibition of tubulin polymerization and anti-angiogenic effects of 15 analogs of 2-methoxyestradiol (1) are reported. The biological studies revealed that the position of nitrogen atom in the heterocyclic ring is important for inhibition of both tubulin polymerization and angiogenesis. The most potent inhibitors were compounds 11f and 13e, with a 6-substituted isoquinoline ring in the 17-position of the steroid skeleton. Moreover, low estrogen activity was observed for the analogs tested at 10 μM concentrations.
Elsevier
以上显示的是最相近的搜索结果。 查看全部搜索结果