Registration Number
0221U107097,
0120U103077
, R & D reports
Title
Interrelations between immunomodulatory and antitumor actions of new heterocyclic compounds (thiazole and 4-thiazolidinone derivatives)
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Head
Lootsik Maxim D., Доктор біологічних наук
Registration Date
26-12-2021
Organization
Institute of Cell Biology of the National Academy of Sciences of Ukraine
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It was investigated 9 new compounds (6 derivatives of 4-thiazolidinone and 3 derivatives of thiazole) for their cytotoxicity towards peripheral blood lymphoid cells of patients with several forms of lymphocytic leukemia and molecular mechanisms of their action. The obtained results indicate that the compounds Les-6287, Les-6294 and U-27971 are the most promising for further study of their antitumor activity. These compounds had a general toxic effect on peripheral blood lymphocytes of acute T-lymphoid leukemia before treatment, chronic lymphocytic leukemia after treatment with bendamustine, chronic lymphocytic leukemia after remission, with a cytotoxicity of IC50 in the range of 0.5-9.6 μM. Peripheral blood lymphocytes in chronic lymphocytic leukemia before treatment were more resistant to the action of derivatives of 4-thiazolidinone and thiazole. Toxic effects of compounds on lymphoid cells were manifested in inhibition / blocking of the cell cycle in the G2-M phase, induction of destructive processes in the cytoplasm by activating apoptosis, the occurrence of breaks in DNA chains with simultaneous inhibition of DNA repair enzymes. Derivatives of 4-thiazolidinone and thiazole showed minor toxicity to mitogen-activated peripheral blood lymphocytes of a clinically healthy donor with an IC50 > 50 μM (for Les-5303, Les-5964, Les-6485) and IC50 > 70 μM (for Les-6287, Les -6294, Les-6295 and U-27971).
Product Description
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Antonyuk Volodymyr Oleksandrovych
Barska Maryna Leonidivna
Klyuchivska Olga Yu.
Lootsik Maxim D.
Senkiv Yuliya V.
Starykovych Marina O.
Stoika Rostyslav Stepanovytch
Finiuk Nataliya S.
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2022-03-09
