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.

引用

页码：2181 / 2184

页数：4

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