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Aliphatic chain-containing macrocycles as diazonamide A analogs
Chemistry of Heterocyclic Compounds ( IF 1.5 ) Pub Date : 2020-06-02 , DOI: 10.1007/s10593-020-02704-6
Viktorija Vitkovska , Rimants Zogota , Toms Kalnins , Diana Zelencova , Edgars Suna

Aliphatic alkyl chain-containing 12–14-membered macrocycles have been designed as structural analogs of antimitotic natural product diazonamide A. Macrocycles were synthesized from 5-bromooxazole in 7 to 9 linear steps using Ru-catalyzed ring-closing metathesis as the key transformation. Heat effect of binding to α,β-tubulin tetramer (T4-RB3 complex) has been measured for the synthesized macrocycles by isothermal titration calorimetry method.


中文翻译:

含脂肪链的大环作为重氮酰胺A类似物

设计了含脂肪族烷基链的12-14元大环化合物作为抗有丝分裂天然产物重氮酰胺A的结构类似物。大环化合物是由5-溴恶唑以7到9个线性步骤合成的,使用Ru催化的闭环复分解为关键转化。通过等温滴定热法测定了合成的大环与α,β-微管蛋白四聚体(T4-RB3配合物)结合的热效应。
更新日期:2020-06-02
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