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ALIPHATIC CHAIN-CONTAINING MACROCYCLES AS DIAZONAMIDE A ANALOGS

Viktorija Vitkovska, Rimants Zogota, Toms Kalnins, Edgars Suna
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Abstract


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.

Keywords


diazonamide A; anticancer agents; macrocycles; ring-closing metathesis.

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