Synthesis and structure-activity relationship of non-peptidic antagonists of neuropilin-1 receptor

LiuW.-Q.; MegaleV.; BorrielloL.; LeforbanB.; MontèsM.; GoldwaserE.; GreshN.; PiquemalJ.-P.; Hadj-SlimaneR.; HermineO.; GarbayC.; RaynaudF.; LepelletierY.; DemangeL.

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Synthesis and structure-activity relationship of non-peptidic antagonists of neuropilin-1 receptor

机译：Neuropilin-1受体非肽拮抗剂的合成及其构效关系

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Neuropilins (NRPs) are VEGF-A165 co-receptors over-expressed in tumor cells, and considered as targets in angiogenic-related pathologies. We previously identified compound 1, the first non-peptidic antagonist of the VEGF-A165/NRP binding, which exhibits in vivo anti-angiogenic and anti-tumor activities. We report here the synthesis and biological evaluations of new antagonists structurally-related to compound 1. Among these molecules, 4a, 4c and 4d show cytotoxic effects on HUVEC and MDA-MB-31 cells, and antagonize VEGF-A165/NRP-1 binding. This study confirmed our key structure-activity relationships hypothesis and paved the way to compound 1 'hit to lead' optimization.

机译：Neuropilins（NRP）是在肿瘤细胞中过度表达的VEGF-A165共受体，被认为是与血管生成相关的病理学的靶标。我们先前确定了化合物1，这是VEGF-A165 / NRP结合的第一个非肽类拮抗剂，它在体内具有抗血管生成和抗肿瘤活性。我们在此报告与化合物1结构相关的新拮抗剂的合成和生物学评估。在这些分子中，4a，4c和4d对HUVEC和MDA-MB-31细胞显示出细胞毒性作用，并拮抗VEGF-A165 / NRP-1的结合。这项研究证实了我们关键的构效关系假设，并为化合物1的“命中率领先”优化铺平了道路。

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《Bioorganic and Medicinal Chemistry Letters》 |2014年第17期|共6页
作者
LiuW.-Q.; MegaleV.; BorrielloL.; LeforbanB.; MontèsM.; GoldwaserE.; GreshN.; PiquemalJ.-P.; Hadj-SlimaneR.; HermineO.; GarbayC.; RaynaudF.; LepelletierY.; DemangeL.;
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正文语种 eng
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Angiogenesis; Docking to receptor; Heterocycles; Neuropilin; Protein-protein interaction;

机译：血管生成;对接受体;杂环;神经氨酸;蛋白-蛋白质相互作用;

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1. Synthesis and structure-activity relationship of non-peptidic antagonists of neuropilin-1 receptor [J] . LiuW.-Q., MegaleV., BorrielloL., Bioorganic and Medicinal Chemistry Letters . 2014,第17期

机译：Neuropilin-1受体非肽拮抗剂的合成及其构效关系
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Synthesis and structure-activity relationship of non-peptidic antagonists of neuropilin-1 receptor

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