Betulinic acid and its derivatives as anti-angiogenic agents

被引：67
|
作者：
Mukherjee, R
Jaggi, M
Rajendran, P
Siddiqui, MJA
Srivastava, SK
Vardhan, A
Burman, AC
机构：
[1] Dabur Res Fdn, Div Expt Oncol, Ghaziabad 201010, Uttar Pradesh, India
[2] Dabur Res Fdn, Chem Res, Ghaziabad 201010, Uttar Pradesh, India
[3] Dabur Res Fdn, Med Chem, Ghaziabad 201010, Uttar Pradesh, India
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 09期
关键词：
D O I：
10.1016/j.bmcl.2004.02.044
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Betulinic acid (1) significantly caused cytotoxicity to endothelial cell line ECV304 (IC50 1.26 +/- 0.44 mug/mL) in a 5-day MTT assay. Novel and more potent derivatives of betulinic acid (2, 4, 6-8) have been synthesized with IC50 less than 0.4 mug/mL. The endothelial cell specificity against human tumor cell lines DU145, L132, A549, and PA-1 were determined. Further betulinic acid (1) inhibited TLS formation of ECV304 cells on Matrigel(TM) by 5.5% while its derivatives caused an inhibition of 13.1-49.2%. (C) 2004 Elsevier Ltd. All rights reserved.
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页码：2181 / 2184
页数：4
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