Synthesis and VEGF inhibitory activity of 16,17-pyrazo-annulated steroids

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 ECs0 values of micromol...

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Bibliographic Details
Published in:Chinese chemical letters 2011-07, Vol.22 (7), p.757-760
Main Authors: Liu, Hong Shan, Zheng, Hu Ling, Ge, Mei, Xia, Peng, Chen, Ying
Format: Article
Language:English
Subjects:
2-Methoxyestradiol (2-ME)
EC50值
Pyrazo-annulated steroid
VEGF
VEGF inhibitory activity
合成
德州仪器
抑制活性
类固醇
血管内皮生长因子
血管内皮细胞生长因子
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Summary: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 ECs0 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.
ISSN:1001-8417
1878-5964
DOI:10.1016/j.cclet.2010.12.043