Antitumor agents 278. 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs as potent in vitro anti-cancer agents

被引：45

作者：

Dong, Yizhou ^{[1
]}

Nakagawa-Goto, Kyoko ^{[1
]}

Lai, Chin-Yu ^{[1
]}

Morris-Natschke, Susan L. ^{[1
]}

Bastow, Kenneth F. ^{[2
]}

Lee, Kuo-Hsiung ^{[1
]}

机构：

[1] Univ N Carolina, Eshelman Sch Pharm, Nat Prod Res Labs, Chapel Hill, NC 27599 USA

[2] Univ N Carolina, Eshelman Sch Pharm, Div Med Chem & Nat Prod, Chapel Hill, NC 27599 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 14期

关键词：

4-Amino-2H-benzo[h]chromen-2-one analogs (ABO); Cytotoxic activity; Structure-activity relationships; BREAST CANCER AGENTS; BIOLOGICAL EVALUATION; NEO-TANSHINLACTONE; NATURAL-PRODUCTS; DERIVATIVES;

D O I：

10.1016/j.bmcl.2010.05.079

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs were designed, synthesized, and evaluated for cytotoxic activity. Among all 4-substituted ABO analogs, cyclohexyl (12), N-methoxy-N-methylacetamide (14), and various aromatic derivatives (15-25 and 27) exhibited promising cell growth inhibitory activity with ED(50) values of 0.01-5.8 mu M against all tested tumor cell lines. The 4'-methoxyphenyl derivative (18) and 3'-methylphenyl derivative (24) showed the most potent antitumor activity against a broad range of cancer cell lines with ED(50) values of 0.01-76 mu M. Preliminary SAR results indicated that substitutions on nitrogen are critical to the antitumor potency. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：4085 / 4087

页数：3

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