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Eur J Med Chem. 2018 Jan 20;144:874-886. doi: 10.1016/j.ejmech.2017.12.040. Epub 2017 Dec 14.

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

Author information

1
Departamento de Antibióticos, Centro de Biociências, Universidade Federal de Pernambuco, 50740-520, Recife, PE, Brazil.
2
Departamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal de Pernambuco, 50740-520, Recife, PE, Brazil.
3
Departamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal de Pernambuco, 50740-520, Recife, PE, Brazil. Electronic address: acllb2003@yahoo.com.br.

Abstract

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.

KEYWORDS:

Cancer; Cell cycle; DNA fragmentation; Mitochondrial depolarization; Thiazoles

PMID:
29329071
DOI:
10.1016/j.ejmech.2017.12.040
[Indexed for MEDLINE]

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