In vivo study of schistosomicidal action of (Z)-1-(2-chloro-6-fluoro-benzyl)-5-thioxo-4-(2,4,6-trimethoxy-benzylidene)-imidazolidin-2-one

Rocha, Thiago José Matos; Lima, Maria Alice Gomes de Andrade; Veras, Dyana Leal; Santos, Aldenir Feitosa dos; Silva, A. L.; Júnior, Antônio Sérgio Alves Almeida; Pitta-Galdino, M. R.; Pitta, Ivan R.; Pitta, M. G. R.; Alves, L. C.; Brayner, Fábio André

doi:10.1590/1519-6984.190062

Cited by 2 publications

(1 citation statement)

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“…A series of imidazolidinone derivatives were reported to be potent phosphodiesterase 4 inhibitors [18]. There has been much research focused on 2-imidazolidinones [19][20][21], but few 4-imidazolidinones have been studied. A previous study reported that 4-imidazolidinone compounds selectively inhibited human neutrophil elastase [22].…”

Section: Discussionmentioning

confidence: 99%

Antiproliferative Evaluation of Novel 4-Imidazolidinone Derivatives as Anticancer Agent Which Triggers ROS-Dependent Apoptosis in Colorectal Cancer Cell

et al. 2022

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Colorectal cancer (CRC) is one of the most common causes of cancer-related death worldwide, and more therapies are needed to treat CRC. To discover novel CRC chemotherapeutic molecules, we used a series of previously synthesized novel imidazolidin-4-one derivatives to study their anticancer role in several cancer cell lines. Among these compounds, compound 9r exhibited the best anticancer activity in CRC cell lines HCT116 and SW620. We further investigated the anticancer molecular mechanism of compound 9r. We found that compound 9r induced mitochondrial pathway apoptosis in HCT116 and SW620 cells by inducing reactive oxygen species (ROS) production. Moreover, the elevated ROS generation activated the c-Jun N-terminal kinase (JNK) pathway, which further accelerated apoptosis. N-acetylcysteine (NAC), an antioxidant reagent, suppressed compound 9r-induced ROS production, JNK pathway activation, and apoptosis. Collectively, this research synthesized a series of imidazolidin-4-one derivatives, evaluated their anticancer activity, and explored the molecular mechanism of compound 9r-induced apoptosis in CRC cells. The present results suggest that compound 9r has a potential therapeutic role in CRC. Hence, it deserves further exploration as a lead compound for CRC treatment.

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Section: Discussionmentioning

confidence: 99%

Antiproliferative Evaluation of Novel 4-Imidazolidinone Derivatives as Anticancer Agent Which Triggers ROS-Dependent Apoptosis in Colorectal Cancer Cell

et al. 2022

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Imidazolidine Derivatives in Cancer Research: What is known?

Júnior

Pitta

Chagas

et al. 2022

ACAMC

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: Even though cancer is the second leading cause of death globally, a number of open issues persist in cancer treatment, despite the achievements of the field. This review aims at discussing the fundamental role of Imidazolidine derivatives in the industry of cancer treatment. Compelling data from 1996 to 2021 will introduce Imidazolidine derivatives as a relevant tool to modulate cancer progression.

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In vivo study of schistosomicidal action of (Z)-1-(2-chloro-6-fluoro-benzyl)-5-thioxo-4-(2,4,6-trimethoxy-benzylidene)-imidazolidin-2-one

Cited by 2 publications

References 9 publications

Antiproliferative Evaluation of Novel 4-Imidazolidinone Derivatives as Anticancer Agent Which Triggers ROS-Dependent Apoptosis in Colorectal Cancer Cell

Antiproliferative Evaluation of Novel 4-Imidazolidinone Derivatives as Anticancer Agent Which Triggers ROS-Dependent Apoptosis in Colorectal Cancer Cell

Imidazolidine Derivatives in Cancer Research: What is known?

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