Pancreatic anticancer activity of a novel geranylgeranylated coumarin derivative

被引：116

作者：

Devji, Tehsina ^{[1
]}

Reddy, Claire ^{[1
]}

Woo, Christina ^{[1
]}

Awale, Suresh ^{[2
]}

Kadota, Shigetoshi ^{[2
]}

Carrico-Moniz, Dora ^{[1
]}

机构：

[1] Wellesley Coll, Dept Chem, Wellesley, MA 02481 USA

[2] Toyama Univ, Inst Nat Med, Toyama 9300194, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 19期

关键词：

Coumarins; Preferential cytotoxicity; Pancreatic cancer; PANC-1; Anticancer agents; NUTRIENT STARVATION; GLUCOSE STARVATION; CANCER-CELLS; TOLERANCE; ELIMINATE; AGENT;

D O I：

10.1016/j.bmcl.2011.08.005

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of hydroxycoumarin derivatives has been synthesized and evaluated against human pancreatic PANC-1 cancer cells under nutrient-deprived conditions. Several compounds exhibited 100% preferential cytotoxicity at low micromolar concentrations under nutrition starvation, and showed no cytotoxicity under nutrient-rich conditions. In this study, a novel geranylgeranylated ether coumarin derivative 9 was found to exhibit the highest cytotoxic activity of 6.25 mu M within 24 h. The preferential anti-tumor activity exhibited by compound 9 against PANC-1 under low oxygen and nutrient environment illustrates its great potential as a promising lead structure for the development of novel agents to combat pancreatic cancer. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：5770 / 5773

页数：4

共 24 条

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