XI-011(XI-011) - 药物靶点：MDMX_在研适应症：乳腺癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

MDMX

作用机制

MDMX抑制剂(Mdm4蛋白抑制剂)

治疗领域

肿瘤皮肤和肌肉骨骼疾病

在研适应症

乳腺癌

非在研适应症-

原研机构

Albany Medical College

在研机构

Albany Medical College

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 XI-011 相关的临床结果

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100 项与 XI-011 相关的转化医学

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100 项与 XI-011 相关的专利（医药）

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1

项与 XI-011 相关的文献（医药）

Molecules

Novel 9-Methylanthracene Derivatives as p53 Activators for the Treatment of Glioblastoma Multiforme

Article

作者: Qiang, Sihan ; Wang, Yingjie ; Wang, Hongbo ; Li, Xiaoxue ; Sun, Ziqiang ; Feng, Yuxin ; Liu, Yi

Glioblastoma multiforme, a highly aggressive and lethal brain tumor, is a substantial clinical challenge and a focus of increasing concern globally. Hematological toxicity and drug resistance of first-line drugs underscore the necessity for new anti-glioma drug development. Here, 43 anthracenyl skeleton compounds as p53 activator XI-011 analogs were designed, synthesized, and evaluated for their cytotoxic effects. Five compounds (13d, 13e, 14a, 14b, and 14n) exhibited good anti-glioma activity against U87 cells, with IC50 values lower than 2 μM. Notably, 13e showed the best anti-glioma activity, with an IC50 value up to 0.53 μM, providing a promising lead compound for new anti-glioma drug development. Mechanistic analyses showed that 13e suppressed the MDM4 protein expression, upregulated the p53 protein level, and induced cell cycle arrest at G2/M phase and apoptosis based on Western blot and flow cytometry assays.

100 项与 XI-011 相关的药物交易

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