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 shu

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

a Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China;
b Laiyi Biological Drug Research and Development Center Co., Ltd., Shanghai 201203, China

Received Date: 12 October 2010

Fund Project: respectively.Thanks are also due to the National Drug Innovative Program (No.2009ZX09301-011) for partial support.This research was supported by grants from the National Natural Science Foundation of China awarded to P.Xia (No.20272010) and Y.Chen (No.30200348 and 30873164)

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.
- Pyrazo-annulated steroid,
- 2-Methoxyestradiol (2-ME),
- VEGF inhibitory activity
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