Structure-Based Design Of Novel Potent Protein Kinase CK2 (CK2) Inhibitors with Phenyl-azole Scaffolds

被引：55

作者：

Hou, Zengye ^{[2
]}

Nakanishi, Isao ^{[1
]}

Kinoshita, Takayoshi

Takei, Yoshinori ^{[2
]}

Yasue, Misato ^{[2
]}

Misu, Ryosuke ^{[2
]}

Suzuki, Yamato ^{[2
]}

Nakamura, Shinya ^{[1
]}

Kure, Tatsuhide ^{[1
]}

Ohno, Hiroald ^{[2
]}

Murata, Katsumi ^{[2
]}

Kitaura, Kazuo ^{[2
]}

Hirasawa, Akira ^{[2
]}

Tsujimoto, Gozoh ^{[2
]}

Oishi, Shinya ^{[2
]}

Fujii, Nobutaka ^{[2
]}

机构：

[1] Kinki Univ, Fac Pharm, Higashiosaka, Osaka 5778502, Japan

[2] Kyoto Univ, Grad Sch Pharmaceut Sci, Sakyo Ku, Kyoto 6068501, Japan

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 55卷 / 06期

关键词：

CELL-SURVIVAL; DERIVATIVES; SUPPRESSOR; TARGET;

D O I：

10.1021/jm2015167

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Protein kinase CK2 (CK2) is a ubiquitous serine/threonine protein kinase for hundreds of endogenous substrates. CK2 has been considered to be involved in many diseases, including cancers. Herein we report the discovery of a novel ATP-competitive CK2 inhibitor. Virtual screening of a compound library led to the identification of a hit 2-phenyl-1,3,4-thiadiazole compound. Subsequent structural optimization resulted in the identification of a promising 4-(thiazol-5-yl)benzoic acid derivative.

引用

页码：2899 / 2903

页数：5

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