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Synthesis, anticancer activity and mechanism of action of new thiazole derivatives

2017; Elsevier BV; Volume: 144; Linguagem: Inglês

10.1016/j.ejmech.2017.12.040

1768-3254

Temístocles Ítalo de Santana, Míria de Oliveira Barbosa, Paulo André Teixeira de Moraes Gomes, Anne Cecília Nascimento da Cruz, Teresinha Gonçalves da Silva, Ana Cristina Lima Leite,

Enzyme function and inhibition

Thiazole derivatives are recognized to possess various biological activities as antiparasitic, antifungal, antimicrobial and antiproliferative. The present work reports the synthesis of 22 new substances belonging to two classes of compounds: thiosemicarbazones and thiazoles, with the purpose of developing new drugs that present high specificity for tumor cells and low toxicity to the organism. A cytotoxic screening was performed to evaluate the performance of the new derivatives in five tumor cell lines. Eight compounds were shown to be promising in at least three tumor cell lines. These compounds had their IC50 determined within 72 h and the activity structure ratio was assessed. The effect of the best compounds on PBMC and hemolytic activity assay was then evaluated. The compound 1d was considered the most promising among the samples tested and its influence on cell cycle, DNA fragmentation and mitochondrial depolarization was evaluated.