14-Aminocamptothecins(14-Aminocamptothecins) - 在研适应症：肿瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Compound 3a(Threshold Pharmaceuticals)

靶点-

作用机制-

治疗领域

肿瘤

在研适应症

肿瘤

非在研适应症-

原研机构

Threshold Pharmaceuticals, Inc.

在研机构

Threshold Pharmaceuticals, Inc.

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-

结构

分子式C20H17N3O4

InChIKeyQIDVDDJMONJMDF-FQEVSTJZSA-N

CAS号1258494-59-5

关联

100 项与 14-Aminocamptothecins 相关的临床结果

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100 项与 14-Aminocamptothecins 相关的转化医学

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100 项与 14-Aminocamptothecins 相关的专利（医药）

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1

项与 14-Aminocamptothecins 相关的文献（医药）

2018-04-01·Bioorganic & Medicinal Chemistry Letters4区 · 医学

Synthesis and biological evaluation of 4,6-diaryl-2-pyrimidinamine derivatives as anti-breast cancer agents

4区 · 医学

Article

作者: You, Qidong ; Tang, Zhichao ; Lu, Xiang ; Wu, Chengze ; Xiang, Hua ; Li, Xinyu ; Huang, Ali ; Liu, Linyi

Breast cancer is the most frequently diagnosed cancers and the leading causes of cancer death among females worldwide. Estrogen receptor positive has been identified as the predominant internal reasons, involving in more than 70% breast cancer patients and SERMs which competes with estradiol for the binding to ERα in breast tissue are widely used in the treatment of ER+ breast cancer, such as tamoxifen, raloxifene. However, many SERMs may cause negative side effects due to their estrogenic activity in other tissues and approximate 50% of patients with ER-positive tumors either initially do not respond or become resistant to these drugs. Here, a series of designed 4,6-diaryl-2-pyrimidinamine derivatives had been synthesized to treat estrogen receptor positive breast cancer by simultaneously antagonizing ER and inhibiting VEGFR-2. Bioactivity evaluation showed that these compounds could significantly inhibit the proliferation of MCF-7, HUVEC and Ishikawa cells. Further studies identified compound III-3A could antagonize against estrogen action and inhibit the phosphorylation of VEGFR-2 as well as inhibit angiogenesis in vivo. The results indicated designed 4,6-diaryl-2-pyrimidinamine derivatives can be used to further study as anti-breast cancer drugs.

100 项与 14-Aminocamptothecins 相关的药物交易

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