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

• Published in: Chinese chemical letters Vol. 22; no. 7; pp. 757 - 760
• Main Authors: Liu, Hong Shan, Zheng, Hu Ling, Ge, Mei, Xia, Peng, Chen, Ying
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.07.2011; Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China%Laiyi Biological Drug Research and Development Center Co., Lid., Shanghai 201203, China
• 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; Pyrazo-annulated steroid; 2-Methoxyestradiol (2-ME); VEGF inhibitory activity
• ISSN: 1001-8417; 1878-5964
• DOI: 10.1016/j.cclet.2010.12.043

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.