HJC-0123(HJC-0123) - 药物靶点：STAT3_专利_临床

概要

基本信息

药物类型

化学药

别名

靶点

STAT3

作用机制

STAT3抑制剂(信号转导和转录激活因子-3抑制剂)

治疗领域

肿瘤消化系统疾病内分泌与代谢疾病+ [1]

在研适应症-

非在研适应症

乳腺癌胰腺癌

原研机构

University of Texas Medical Branch

在研机构-

非在研机构

University of Texas Medical Branch

最高研发阶段无进展药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C24H16N2O3S

InChIKeyZUYCAEIBKWUMND-UHFFFAOYSA-N

CAS号1430420-02-2

关联

100 项与 HJC-0123 相关的临床结果

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100 项与 HJC-0123 相关的转化医学

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100 项与 HJC-0123 相关的专利（医药）

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2

项与 HJC-0123 相关的文献（医药）

2013-04-01·European Journal of Medicinal Chemistry1区 · 医学

Fragment-based drug design and identification of HJC0123 , a novel orally bioavailable STAT3 inhibitor for cancer therapy

1区 · 医学

Article

作者: Qiang Shen ; Zhengduo Yang ; Chunyong Ding ; Huiling Liu ; Jia Zhou ; Haijun Chen ; Kristin Terry ; Lili Chu ; Yusong Zhang

Fragment-based drug design (FBDD) is a promising approach for the generation of lead molecules with enhanced activity and especially drug-like properties against therapeutic targets. Herein, we report the fragment-based drug design, systematic chemical synthesis and pharmacological evaluation of novel scaffolds as potent anticancer agents by utilizing six privileged fragments from known STAT3 inhibitors. Several new molecules such as compounds 5, 12, and 19 that may act as advanced chemical leads have been identified. The most potent compound 5 (HJC0123) has demonstrated to inhibit STAT3 promoter activity, downregulate phosphorylation of STAT3, increase the expression of cleaved caspase-3, inhibit cell cycle progression and promote apoptosis in breast and pancreatic cancer cells with low micromolar to nanomolar IC50 values. Furthermore, compound 5 significantly suppressed estrogen receptor (ER)-negative breast cancer MDA-MB-231 xenograft tumor growth in vivo (p.o.), indicating its great potential as an efficacious and orally bioavailable drug candidate for human cancer therapy.

RSC Advances3区 · 化学

STAT3 inhibition suppresses hepatic stellate cell fibrogenesis: HJC0123, a potential therapeutic agent for liver fibrosis

3区 · 化学

ArticleOA

作者: Chen, Haijun ; Radhakrishnan, Ravi S. ; Chen, Haiying ; Corsello, Tiziana ; Nunez Lopez, Omar ; Wang, Xiaofu ; Zhou, Jia ; Bohanon, Fredrick J. ; Ye, Na ; Rojas-Khalil, Yesenia

The novel small molecule HJC0123 will inhibit STAT3 activation in human HSCs resulting in decreased fibrogenesis, unveiling a potential role for its use as a therapeutic agent for the treatment of liver fibrosis.

100 项与 HJC-0123 相关的药物交易

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