4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors

被引：40

作者：

Ishida, J

Hattori, K

Yamamoto, H

Iwashita, A

Mihara, K

Matsuoka, N

机构：

[1] Med Chem Res Labs, Yodogawa Ku, Osaka 5328514, Japan

[2] Fujisawa Pharmaceut Co Ltd, Med Biol Res Labs, Yodogawa Ku, Osaka 5328514, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 19期

关键词：

PARP-1; poly(ADP-ribose) polymerase; 4-phenyl-1,2,3,6-tetrahydropyridine;

D O I：

10.1016/j.bmcl.2005.06.094

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have shown that a 4-phenyl-1,2,3,6-tetrahydropyridine fragment plays an important role in improving inhibitory potency against poly(ADP-ribose) polymerise-1 (PARP-1). Various benzamide analogues linked with this fragment via alkyl spacers have been prepared and evaluated. As a result, some of them have been found to be highly potent PARP-1 inhibitors. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：4221 / 4225

页数：5

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