SB-639(SB-639) - 药物靶点：HDACs_专利_临床

概要

基本信息

药物类型

化学药

别名

SB 639、SB639

靶点

HDACs

作用机制

HDAC抑制剂(组蛋白去乙酰化酶家族抑制剂)

治疗领域

肿瘤消化系统疾病

在研适应症-

非在研适应症

结肠癌

原研机构

S*BIO Pte Ltd.

在研机构-

非在研机构

S*BIO Pte Ltd.

MEI Pharma, Inc.

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 SB-639 相关的临床结果

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100 项与 SB-639 相关的转化医学

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100 项与 SB-639 相关的专利（医药）

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1

项与 SB-639 相关的文献（医药）

2009-03-01·Bioorganic & medicinal chemistry letters4区 · 医学

N-Hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides as novel histone deacetylase inhibitors: Design, synthesis, SAR studies, and in vivo antitumor activity

4区 · 医学

Article

作者: Weiping Deng ; Niefang Yu ; Xukun Wang ; Zahid Bonday ; Joyce Chang ; Kanda Sangthongpitag ; Anders Poulsen ; Eric T. Sun ; Yong Zou ; Hongyan Song ; Pek Ling Lye ; Siok Kun Goh ; Stéphanie Blanchard ; Michael Entzeroth ; Dizhong Chen ; Haishan Wang ; Xiaofeng Wu ; Kee Chuan Goh ; Wai Chung Ong ; Hwee Hoon Khng ; Melvin Ng ; Walter Stünkel ; Lijuan Fang

A series of N-hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides were designed and synthesized as novel HDAC inhibitors. General SAR has been established for the substituents at positions 1 and 2, as well as the importance of the ethylene group and its attachment to position 5. Optimized compounds are much more potent than SAHA in both enzymatic and cellular assays. A representative compound, 23 (SB639), has demonstrated antitumor activity in a colon cancer xenograft model.

100 项与 SB-639 相关的药物交易

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