Biopolym. Cell. 2021; 37(4):303-314.
Біоорганічна хімія
Оцінка антипроліферативної активності вибраних 1,2,3-триазол-4-карбонових кислот — ключових фрагментів та попередників протипухлинних 1,2,3-триазол-4-карбоксамідів
1Походило Н. Т., 1Матійчук В. С.
  1. Львівський національний університет імені Івана Франка
    вул. Кирила і Мефодія, 6, Львів, Україна, 79005

Abstract

Мета. Оцінити in vitro антипроліферативну дію відібраних 1,2,3-триазол-карбонових кислот, які є ключових фрагментами та попередниками протипухлинних 1,2,3-триазол-4-карбоксамідів. Методи. Органічний синтез, аналіз цитотоксичності in vitro, аналіз МТТ, спектрофотометрія, статистичний аналіз. Результати. Відібрані 1,2,3-триазол-4-карбонові кислоти та їх ефіри, синтезовані відповідно до зручної синтетичної процедури, були протестовані на їх протипухлинну активність на 60 лініях ракових клітин. Попередні результати дозволили виявити найбільш активні сполуки та знайти взаємозв’язок між структурою та активністю. Найбільш активні 1,2,3-триазол-4-карбонові кислоти обрані, як перспективні для проектування 1,2,3-триазол-4-карбоксамідів для скринінгу протипухлинної активності. Висновки. Отримані результати протипухлинної активності таких похідних цікаві для відкриття активних протипухлинних агентів серед 1,2,3-триазол-4-карбоксамідів з точки зору концепції фрагмент-орієнтованого дизайну лікарських засобові (FBDD) та підтверджують необхідність подальших досліджень.
Keywords: 1,2,3-триазоли, 1,2,3-триазол-4-карбоксаміди, 1,2,3-триазол-4-карбонові кислоти, протипухлинна активність, клітинна проліферація

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