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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis and in vitro evaluation of (18F)fluoroethyl triazole labelled (Tyr3)octreotate analogues using click chemistry.
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Synthesis and in vitro evaluation of (18F)fluoroethyl triazole labelled (Tyr3)octreotate analogues using click chemistry.

机译：（18F）氟乙基三唑标记的（Tyr3）奥曲肽类似物的合成和体外评价使用点击化学。

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摘要

A novel class of alkyne linked [Tyr(3)]octreotate analogues have been labelled by a copper catalysed azide-alkyne cycloaddition reaction (CuAAC) to form a 1,4-substituted triazole using the reagent [(18)F]2-fluoroethyl azide. An unexpected variability in reactivity during the CuAAC reaction was observed for each alkyne analogue which has been investigated. Two lead alkyne linked [Tyr(3)]octreotate analogues, G-TOCA (3a) and betaAG-TOCA (5a) have been identified to be highly reactive in the click reaction showing complete conversion to the [(18)F]2-fluoroethyl triazole linked [Tyr(3)]octreotate analogues FET-G-TOCA (3b) and FET-betaAG-TOCA (5b) under mild conditions and with short synthesis times (5 min at 20 degrees C). As well as ease of synthesis, in vitro binding to the pancreatic tumour AR42J cells showed that both FET-G-TOCA and FET-betaAG-TOCA have high affinity for the somatostatin receptor with IC(50) of 4.0+/-1.4, and 1.6+/-0.2 nM, respectively.
机译：新型的炔烃连接的[Tyr（3）]奥曲肽类似物已通过铜催化的叠氮化物-炔烃环加成反应（CuAAC）进行了标记，从而使用试剂[（18）F] 2-氟乙基形成了1,4-取代的三唑叠氮化物。对于每个已研究的炔烃类似物，在CuAAC反应过程中观察到了反应性的意外变化。两个铅炔烃连接的[Tyr（3）]奥曲肽类似物G-TOCA（3a）和betaAG-TOCA（5a）已被确定在点击反应中具有高反应性，表明已完全转化为[（18）F] 2-氟乙基三唑在温和的条件下且合成时间短（在20摄氏度下5分钟）连接[Tyr（3）]奥曲肽类似物FET-G-TOCA（3b）和FET-betaAG-TOCA（5b）。除了易于合成外，体外结合胰腺肿瘤AR42J细胞还显示FET-G-TOCA和FET-betaAG-TOCA对生长抑素受体均具有高亲和力，IC（50）为4.0 +/- 1.4，并且分别为1.6 +/- 0.2 nM。

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