Synthesis and cytotoxic activity of 3-O-acyl/3-hydrazine/2-bromo/20,29-dibromo betulinic acid derivatives

被引：37

作者：

Mukherjee, R

Jaggi, M

Siddiqui, MJA

Srivastava, SK

Rajendran, P

Vardhan, A

Burman, AC

机构：

[1] Dabur Res Fdn, Div Expt Oncol, Ghaziabad 201010, Uttar Pradesh, India

[2] Dabur Res Fdn, Div Chem Res, Ghaziabad 201010, Uttar Pradesh, India

[3] Dabur Res Fdn, Div Med Chem, Ghaziabad 201010, Uttar Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 15期

关键词：

D O I：

10.1016/j.bmcl.2004.05.034

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

A series of 3-O-acyl, 3-hydrazine, 2-bromo, and 20,29-dibromo betulinic acid derivatives (1-27) have been synthesized and screened for in vitro cytotoxic activity on human cancer cell lines MOLT-4, JurkatE6.1, CEM.CM3, BRISTOL8, U937, DU145, PA-1 A549, and L132. A number of compounds have shown ED50 < 1 mug/mL against the cancer cell lines tested and have shown better cytotoxicity than betulinic acid. Compounds 13, 19, 20, 23, and 27 were the best derivatives and were selected as lead molecules for further development. The structure-activity relationship has been described. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：4087 / 4091

页数：5

共 19 条

[1]

Chemistry, biological activity, and chemotherapeutic potential of betulinic acid for the prevention and treatment of cancer and HIV infection [J].