引用本文:
Hong Shan Liu, Hu Ling Zheng, Mei Ge, Peng Xia, Ying Chen. Synthesis and VEGF inhibitory activity of 16,17-pyrazo-annulated steroids[J]. Chinese Chemical Letters,
2011, 22(7): 757-760.
doi:
10.1016/j.cclet.2010.12.043
Citation: Hong Shan Liu, Hu Ling Zheng, Mei Ge, Peng Xia, Ying Chen. Synthesis and VEGF inhibitory activity of 16,17-pyrazo-annulated steroids[J]. Chinese Chemical Letters, 2011, 22(7): 757-760. doi: 10.1016/j.cclet.2010.12.043
Citation: Hong Shan Liu, Hu Ling Zheng, Mei Ge, Peng Xia, Ying Chen. Synthesis and VEGF inhibitory activity of 16,17-pyrazo-annulated steroids[J]. Chinese Chemical Letters, 2011, 22(7): 757-760. doi: 10.1016/j.cclet.2010.12.043
Synthesis and VEGF inhibitory activity of 16,17-pyrazo-annulated steroids
摘要:
Eight 16,17-pyrazo-annulated steroidal derivatives were synthesized and evaluated in vitro vascular endothelial growth factor (VEGF) inhibitory activity with 2-methoxyestradiol (2-ME) as the reference compound. Most of the compounds showed potent VEGF inhibitory activity with EC50 values of micromolar or submicromolar range. Among them, the compounds 3 and 8 exhibited similar EC50 values and obviously better TI values compared with 2-ME.
English
Synthesis and VEGF inhibitory activity of 16,17-pyrazo-annulated steroids
Abstract:
Eight 16,17-pyrazo-annulated steroidal derivatives were synthesized and evaluated in vitro vascular endothelial growth factor (VEGF) inhibitory activity with 2-methoxyestradiol (2-ME) as the reference compound. Most of the compounds showed potent VEGF inhibitory activity with EC50 values of micromolar or submicromolar range. Among them, the compounds 3 and 8 exhibited similar EC50 values and obviously better TI values compared with 2-ME.
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