Ukr.Biochem.J. 2020; Том 92, № 2, березень-квітень, c. 108-119

doi: https://doi.org/10.15407/ubj92.02.108

Синтез та протилейкемічна активність піролідиндіон-тіазолідинонових гібридів

A. Крищишин1*, Д. Камінський1, О. Роман1,
Р. Краловіч2, О. Карпенко3, Р. Лесик1

1Кафедра фармацевтичної, органічної і біоорганічної хімії, Львівський національний медичний університет імені Данила Галицького, Україна;
2Центр досліджень молекулярної медицини, Австрійська академія наук, Відень, Австрія;
3ТзОВ Енамін, Київ, Україна;
*e-mail: kryshchyshyn.a@gmail.com

Отримано:  22 грудня 2019; Затверджено: 27 березня 2020

Розроблено дизайн структури та синтезовано ряд нових 2-(5-іліден-4-оксо-2-тіоксотіазоілдин-3-іл)-сукцинімідів та 5-іліден-3-(1-арилпіролідин-2,5-діон)-тіазоілдин-2,4-діонів. Запропоновано ефективний простий метод синтезу роданін-піролідиндіонових гібридів, що дає змогу уникнути стадії утворення ангідриду. Зважаючи­ на попередні дані щодо протилейкемічної активності споріднених похідних тіазолі­динону, біологічна активність цільових сполук досліджувалася на клітинних лініях Dami, HL-60, Jurkat та K562. Серед досліджених сполук, ідентифіковано 3-[5-(4-хлоробензиліден)-4-оксо-2-тіоксотіазолідин-3-іл]-1-фенілпіролідин-2,5-діон, що володіє доброю і селективною антипроліферативною активністю на лініях Dami та HL-60, а також задовільними токсикологічними параметрами (гостра токсичність in vivo).

Ключові слова: , , ,


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