Novel semisynthetic spin-labeled derivatives of podophyllotoxin with cytotoxic and antioxidative activity

被引：21

作者：

Zhang, Jia-Qiang ^{[1
]}

Zhang, Zhi-Wei ^{[1
]}

Hui, Ling ^{[3
]}

Chen, Shi-Wu ^{[1
,2
]}

Tian, Xuan ^{[1
]}

机构：

[1] Lanzhou Univ, State Key Lab Appl Organ Chem, Lanzhou 730000, Peoples R China

[2] Lanzhou Univ, Sch Pharm, Lanzhou 730000, Peoples R China

[3] Lanzhou Gen Hosp, Ctr Med Expt, Lanzhou 730050, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 03期

关键词：

Podophyllotoxin; Nitroxides; Antitumor; Antioxidants; BIOLOGICAL EVALUATION; ANTITUMOR-ACTIVITY; DESIGN; ASSAY;

D O I：

10.1016/j.bmcl.2009.12.048

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel spin-labeled podophyllotoxin derivatives were synthesized by reacting the corresponding N-(1-oxyl-2,2,6,6-tetramethyl-4-piperidinyloxy carbonyl)-amino acids with 4 beta-amino-4'-demethylepipodophyllotoxin. The synthesized derivatives 12a-g were evaluated for the partition coefficients, cytotoxicities in vitro against three tumor cell lines (A-549, HL-60, and RPMI-8226) and antioxidative activities in tissues of SD rats by the TBA method. The vast majority of target compounds have shown superior or comparable activities against A-549, HL-60, and RPMI-8226 compared to VP-16, and they have shown more significant antioxidative activities and superior water solubility than VP-16. (c) 2009 Elsevier Ltd. All rights reserved.

引用

页码：983 / 986

页数：4

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