Biopolym. Cell. 2020; 36(6):466-476.
http://dx.doi.org/10.7124/bc.000A44
Біоорганічна хімія
Синтез 5-гетариламіно-3-арил-1H-індазолів як інгібіторів протеїнкінази CK2
1Протопопов М. В., 1Вдовін В. С., 1Лукашов С. С., 1Остринська О. В., 1, 2Борисенко І. П., 1Боровиков О. В., 1Старосила С. А., 3Білокінь Я. В., 1Кухаренко О. П., 1Бджола В. Г., 1Ярмолюк С. М.
  1. Інститут молекулярної біології і генетики НАН України
    Вул. Академіка Заболотного, 150, Київ, Україна, 03143
  2. Фірма “Otava”
    Вул. Академіка Заболотного, 150, Київ, Україна, 03143
  3. OTAVA Ltd
    400 Applewood Crescent, блок 100, Vaughan, Онтаріо, Канада L4K 0C3

Abstract

Мета. В продовження пошуку нових інгібіторів протеїнкінази CK2 грунтуючись на раніше виявленій нами інгібуючій активності похідних 5-(4-хіназоліламіно)-3-ариліндазолу було виконано синтез нових азотвмісних гетероциклічних похідних 5-аміно-3-арил-індазолу. Методи. Органічний синтез, спектроскопія ЯМР. Результати. Було синтезовано низку 4-хлорохіназолінів, 4-хлорохінолінів, 4-хлоропіразоло[3,4-d]піримідинів та 4-хлоротієно[2,3-d]піримідин. Взаємодією цих інтермедіатів з 5-аміно-3-(3,4-дихлорфеніл)-індазолом було одержано 14 нових гетероциклічних похідних 5-аміно-3-(3,4-дихлорфеніл)-індазолу. Висновки. Крім нових похідних хіназолину, було отримано похідні хіноліну та тієно[2,3-d]піримідину близькі за структурою, але відмінні за полярністю. Також було синтезовано низку 1-метилпіразоло[3,4-d]піримідинових похідних зі зниженою ліпофільністю.
Keywords: синтез, індазол, хіназолін, тієно[2,3-d]піримідин, піразоло[3,4-d]піримідин, інгібітор протеїнкінази CK2
Повний текст: (PDF, англійською)

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