Synthesis of 4-(4-chlorophenyl)thiazole compounds: in silico and in vitro evaluations as leishmanicidal and trypanocidal agents

Filho, Iranildo José da Cruz; Oliveira, Jamerson Ferreira de; Santos, Aline Caroline da Silva; Pereira, Valéria Rêgo Alves; Lima, Manfredo

doi:10.1590/0001-3765202320220538

Cited by 1 publication

(8 citation statements)

References 49 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The in vitro toxicity tests promoted by thiosemicarbazones were carried out according to Jacob et al (2023) with few modifications. The normal cell lines used were: J774 macrophages (strain An Acad Bras Cienc (2024) 96(2) e20231247 4 | 19 obtained from mice), Vero cells (renal epithelial cells extracted from an African green monkey) and V79 fibroblasts (cells obtained from the lung tissue of a Chinese hamster).…”

Section: In Vitro Toxicity Tests Against Normal and Tumor Cell Linesmentioning

confidence: 99%

“…The in vitro hemolytic activity assays were performed according to the methodology proposed by Cruz Filho et al (2023) and Jacob et al (2023) respectively. Erythrocytes were isolated by centrifugation under the following conditions: 2000 rpm, 15 min at 4 °C and the supernatant was removed.…”

Section: In Vitro Hemolytic Activitymentioning

confidence: 99%

“…The evaluation of in vitro antioxidant activity was performed according to the methodology proposed by Jaishree et al ( 2012 2023) and Jacob et al (2023) respectively. In this study, the tests performed were: capture of DPPH, ABTS, hydroxyl radicals (OH), nitric oxide (NO) and reduction of iron ions.…”

Section: In Vitro Antioxidant Activity Assaysmentioning

confidence: 99%

“…The cancers that most caused death in the respective year were: lung, colon and rectum, liver, stomach and breast respectively (Morgan et al 2023, Shafiee et al 2023. In Brazil, 704,000 new cases of cancer are expected for the three-year period [2023][2024][2025] (Oliveira Santos et al 2023).…”

Section: Introductionmentioning

confidence: 99%

“…Thiosemicarbazones and their structural analogues are known in the literature for having different biological and pharmacological activities (Jacob et al 2023). Regarding the antitumor activities promoted by different thiosemicarbazones, we will cite the works carried out by Bai et al (2022) and Chaudhary et al (2022), Jacob et al (2023). The authors verified that thiosemicarbazones are potential drug candidates and that they showed promising results, that is, the compounds were less toxic for mammalian cells and more toxic for tumor cells, an important prerequisite for the screening of chemotherapy drugs.…”

Section: Introductionmentioning

confidence: 99%

See 4 more Smart Citations

Preliminary evaluation of the toxicological, antioxidant and antitumor activities promoted by the compounds 2,4-dihydroxy-benzylidene-thiosemicarbazones an in silico, in vitro and in vivo study

LEAL,

SILVA,

MARQUES

et al. 2024

An. Acad. Bras. Ciênc.

View full text Add to dashboard Cite

Thiosemicarbazones are promising classes of compounds with antitumor activity. For this study, six 2,4-dihydroxy-benzylidene-thiosemicarbazones compounds were synthesized. These compounds were submitted to different assays in silico, in vitro and in vivo to evaluate the toxicological, antioxidant and antitumor effects. The in silico results were evaluated by the SwissADME and pkCSM platforms and showed that all compounds had good oral bioavailability profiles. The in vitro and in vivo toxicity assays showed that the compounds showed low cytotoxicity against different normal cells and did not promote hemolytic effects. The single dose acute toxicity test (2000 mg/kg) showed that none of the compounds were toxic to mice. In in vitro antioxidant activity assays, the compounds showed moderate to low activity, with PB17 standing out for the ABTS radical capture assay. The in vivo antioxidant activity highlighted the compounds 1, 6 and 8 that promoted a significant increase in the concentration of liver antioxidant enzymes. Finally, all compounds showed promising antitumor activity against different cell lines, especially MCF-7 and DU145 lines, in addition, they inhibited the growth of sarcoma 180 at concentrations lower than 50 mg/kg. These results showed that the evaluated compounds can be considered as potential antitumor agents.

show abstract

Section: In Vitro Toxicity Tests Against Normal and Tumor Cell Linesmentioning

confidence: 99%

Section: In Vitro Hemolytic Activitymentioning

confidence: 99%

Section: In Vitro Antioxidant Activity Assaysmentioning

confidence: 99%