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4-[(N-Imidazol-2-ylmethyl)anilino]pyranopyridine Analogs as Novel Anti-Angiogenic Agents

机译:4-[(N-咪唑-2-基甲基)苯胺基]吡喃吡啶类似物作为新型抗血管生成剂

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摘要

We attempted to replace a benzopyran ring of 4-[(N-imidazol-2-ylmethyl)-4-chloroanilino]benzopyran,previously discovered as anti-angiogenic agent with antitumor activity,with pyranopyridines.The [3,2-c]-,[3,2-b]-,[2,3-c]-,and [2,3-b]-pyranopyridines with N-(imidazol-2-ylmethyl)aniline moiety at the 4-position,were synthesized respectively,and evaluated for primary anti-angiogenic properties through primary cultured HUVEC tube formation assay.From this study,we found that the pyranopyridine ring,especially [3,2-b]-and [2,3-c]-isomer,can replace the benzopyran ring of the compound 1 and can be optimized through the introduction of substituents both on the pyranopyridine ring and the aniline moiety for the identification of a novel anti-angiogenic agent.
机译:我们试图用吡喃吡啶取代4-[(N-咪唑-2-基甲基)-4-氯苯胺基]苯并吡喃的苯并吡喃环,吡喃并吡啶是具有抗肿瘤活性的抗血管生成剂。[3,2-c]-分别合成了在4-位具有N-(咪唑-2-基甲基)苯胺部分的[3,2-b]-,[2,3-c]-和[2,3-b]-吡喃吡啶并通过原代培养的HUVEC管形成试验评估了其主要的抗血管生成特性。从这项研究中,我们发现吡喃并吡啶环,特别是[3,2-b]-和[2,3-c]-异构体可以替代化合物1的苯并吡喃环,并且可以通过在吡喃吡啶环和苯胺部分上引入取代基来优化,以鉴定新型抗血管生成剂。

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