Thienopyridine and benzofuran derivatives as potent anti-tumor agents possessing different structure-activity relationships

被引：124

作者：

Hayakawa, I

Shioya, R

Agatsuma, T

Furukawa, H

Sugano, Y ^{[1
]}

机构：

[1] Sankyo Co Ltd, Lead Discovery Res Labs, Shinagawa Ku, Tokyo 1408710, Japan

[2] Sankyo Co Ltd, Biomed Res Labs, Shinagawa Ku, Tokyo 1408710, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 13期

关键词：

lead compound; SAR; anticancer;

D O I：

10.1016/j.bmcl.2004.04.079

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

(3 -Amino-6-thiophen-2-yl-thieno[2,3 -b]pyridin-2-yl)phenylmethanone (3) was discovered as a new type of cytotoxic agent selective against a tumorigenic cell line. The molecular structure of a previously reported compound, (4-hydroxy-3-methyl-6-phenylbenzofuran-2-yl)phenylmethanone (2), had remarkably similar bioisosteric substructures to that of compound 3. Although the relationship between the molecular structure and biological activity of each derivative synthesized from these two hit compounds (2 and 3) were studied, unexpectedly no correlation was observed. However, after further synthetic study from 3, one of the most potent derivative (10k) having a different SAR profile from 2, was discovered. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：3411 / 3414

页数：4