Ellipravin(Ellipravin) - _专利_临床

概要

基本信息

药物类型

小分子化药

别名

Elliprabin

靶点-

作用机制-

治疗领域

肿瘤

在研适应症-

非在研适应症

肿瘤

原研机构

Asubio Pharma Co. Ltd.

在研机构-

非在研机构

Suntory Holdings Ltd.Asubio Pharma Co. Ltd.

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C22H23BrN2O5

InChIKeyOKNKQPUDKRCBIK-MAVIPZKQSA-N

CAS号103461-20-7

关联

100 项与 Ellipravin 相关的临床结果

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100 项与 Ellipravin 相关的转化医学

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100 项与 Ellipravin 相关的专利（医药）

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2

项与 Ellipravin 相关的文献（医药）

1997-01-01·Chemical and Pharmaceutical Bulletin4区 · 医学

Synthesis and Antitumor Activity of Quaternary Salts of 2-(2'-Oxoalkoxy)-9-hydroxyellipticines.

4区 · 医学

Article

作者: Hashiyama, Tomiki ; Tsujihara, Kenji ; Oda, Kouji ; Harada, Naoyuki ; Kawaguchi, Takayuki ; Inoue, Isao ; Ohashi, Motoaki

Various kinds of water-soluble quaternary salts of 2-(2'-oxoalkoxy)-9-hydroxyellipticines were synthesized in a search for compounds with potent antitumor activity and low toxicity. Some compounds exhibited more potent antitumor activities than elliptinium (1) and SUN 4599 (3). In particular, 2-(3'-methoxy-2'-oxopropanoxy)-9- hydroxy-5,11-dimethyl-6H-pyrido[4,3-b]carbazolium bromide (4d) showed potent antitumor activities against P388 leukemia, colon 26, and Lewis lung carcinoma.

1995-09-01·Japanese Journal of Cancer Research

Inhibition of p53 Protein Phosphorylation by 9‐Hydroxyellipticine: A Possible Anticancer Mechanism

Article

作者: Emiko Sugikawa ; Noriyuki Nakanishi ; Motoaki Ohashi

Abnormality of p53, a tumor suppressor gene, is considered to be a potential cause of malignancy. We found that ellipticine and 9‐hydroxyellipticine (9HE), antitumor alkaloids, caused selective inhibition of p53 protein phospborylation in Lewis lung carcinoma and SW480 (human colon cancer cell line) in a concentration‐dependent manner from 0.1 to 100 μM. 9HE suppressed cdk2 kinase activity concentration‐dependently from 1 to 100 μM. By contrast, the inhibition of p53 protein phosphorylation by elliptinium and elliprabin (N2 substituted derivatives of 9HE) was very weak. A good correlation was observed between p53 phosphorylation inhibition and cytotoxic activity of these agents in terms of concentration‐response relationships, suggesting that inhibition of p53 protein phosphorylation via kinase inhibition may be involved in the anticancer mechanism of these agents. In addition, this study demonstrated that brief exposure to 9HE caused apoptosis of cancer cells. It is suggested that accumulation of dephosphorylated mutant p53 may induce apoptosis.

100 项与 Ellipravin 相关的药物交易

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