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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Amide-sulfamide modulators as effective anti-tumor metastatic agents targeting CXCR4/CXCL12 axis
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Amide-sulfamide modulators as effective anti-tumor metastatic agents targeting CXCR4/CXCL12 axis

机译：酰胺 - 磺酰胺调节剂是靶向CXCR4 / CXCL12轴的有效抗肿瘤转移剂

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Breast cancer is the most frequently diagnosed malignancy and the second common cause of death in women worldwide. High mortality in breast cancer is frequently associated with metastatic progression rather than the primary tumor itself. It has been recently identified that the CXCR4/CXCL12 axis plays a pivotal role in breast cancer metastasis, especially in directing metastatic cancer cells to CXCL12-riched organs and tissues. Herein, taking the amide-sulfamide as the lead structure, the second-round structural modifications to the sulfamide structure were performed to obtain more active CXCR4 modulators against tumor metastasis. Both in vivo and in vitro experiments illustrated that compound he possessed potent CXCR4 binding affinity, excellent anti-metastatic and anti-angiogenetic activity against breast cancer. More importantly, in a mouse breast cancer lung metastasis model, compound Me exerted a significant inhibitory effect on breast cancer metastasis. Taken together, all these positive results demonstrated that developing of CXCR4 modulators is a promising strategy to mediate breast cancer metastasis. (C) 2019 Elsevier Masson SAS. All rights reserved.
机译：乳腺癌是全世界妇女死亡最常诊断的恶性肿瘤和第二常见的死因。乳腺癌的高死亡率通常与转移性进展而不是原发性肿瘤本身有关。最近发现CXCR4 / CXCL12轴在乳腺癌转移中发挥枢转作用，特别是在将转移性癌细胞引导至CXCL12富含器官和组织中。在此，取酰胺 - 磺酰胺作为铅结构，进行对磺酰胺结构的第二圆形结构修饰，以获得针对肿瘤转移的更活跃的CXCR4调节剂。体内和体外实验中的两者都示出了他具有有效的CXCR4结合亲和力，优异的抗转移性和抗血管生成活性对乳腺癌具有效率。更重要的是，在小鼠乳腺癌肺转移模型中，化合物我对乳腺癌转移产生了显着的抑制作用。占据了所有这些阳性结果表明，CXCR4调节剂的发展是介导乳腺癌转移的有希望的策略。 （c）2019年Elsevier Masson SAS。版权所有。

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