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Chem Biol Interact ; 347: 109597, 2021 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-34303695

RESUMO

In this work, 22 new compounds were obtained and evaluated for their cytotoxic activity on peripheral blood mononuclear cells (PBMC) and eight different tumor cell lines. All compounds displayed IC50 values above 100 µM when assayed against PBMCs. The cytotoxic assays in tumor cell lines revealed that sub-series of phthalimido-bis-1,3-thiazoles (5a-f) exhibited the best anti-tumor activity profile, presenting viability values below 59 %. As a result, the IC50 value was calculated for compounds 5a-f and 4c, and compounds 5b and 5e were selected for further assays due to their best IC50s. Considering the results presented by the sub-series 5a-f, the importance of the 1,3-thiazole ring in improving the anti-tumor activity was pointed out. Together, the results highlighted the anti-tumor activity of phthalimido-bis-1,3-thiazole derivatives.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Tiazóis/síntese química , Tiazóis/farmacologia , Linhagem Celular , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais/métodos , Células HL-60 , Humanos , Células K562 , Leucócitos Mononucleares/efeitos dos fármacos , Estrutura Molecular , Relação Estrutura-Atividade
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