Abstract Cancer is a complex and multifactorial disease characterized by uncontrolled cell growth and is one of the main causes of death in the world. This work aimed to evaluate a small series of 10 different indole-thiosemicarbazone compounds as potential antitumor agents. This is a pioneering study. For this, the antioxidant and cytotoxic capacity against normal and tumor cells was evaluated. The results showed that the compounds were able to promote moderate to low antioxidant activity for the ABTS radical scavenging assay. ADMET in silico assays showed that the compounds exhibited good oral bioavailability. As for toxicity, they were able to promote low cytotoxicity against normal cells, in addition to not being hemolytic. The compounds showed promising in vitro antitumor activity against the T47D, MCF-7, Jurkat and DU-145 strains, not being able to inhibit the growth of the Hepg2 strain. Through this in vitro study, it can be concluded that the compounds are potential candidates for antitumor agents. world 1 indolethiosemicarbazone indole thiosemicarbazone agents study evaluated assay bioavailability toxicity hemolytic T47D TD T D MCF7, MCF7 MCF 7, 7 MCF-7 DU145 DU 145 DU-14 strains Hepg strain MCF- DU14 14 DU-1 DU1 DU-

Abstract 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. study 2,4dihydroxybenzylidenethiosemicarbazones 24dihydroxybenzylidenethiosemicarbazones dihydroxybenzylidenethiosemicarbazones 2,4 dihydroxy benzylidene thiosemicarbazones 2 4 synthesized toxicological effects profiles 2000 (200 mg/kg mgkg mg kg mice PB PB1 assay 1 enzymes Finally lines MCF7 MCF 7 MCF- DU DU14 addition 18 5 agents 4dihydroxybenzylidenethiosemicarbazones 24 2, 200 (20 DU1 20 (2 (

Abstract Neglected tropical diseases are a diverse group of communicable pathologies that mainly prevail in tropical and subtropical regions. Thus, the objective of this work was to evaluate the biological potential of eight 4-(4-chlorophenyl)thiazole compounds. Tests were carried out in silico to evaluate the pharmacokinetic properties, the antioxidant, cytotoxic activities in animal cells and antiparasitic activities were evaluated against the different forms of Leishmania amazonensis and Trypanosoma cruzi in vitro. The in silico study showed that the evaluated compounds showed good oral availability. In a preliminary in vitro study, the compounds showed moderate to low antioxidant activity. Cytotoxicity assays show that the compounds showed moderate to low toxicity. In relation to leishmanicidal activity, the compounds presented IC50 values that ranged from 19.86 to 200 µM for the promastigote form, while for the amastigote forms, IC50 ranged from 101 to more than 200 µM. The compounds showed better results against the forms of T. cruzi with IC50 ranging from 1.67 to 100 µM for the trypomastigote form and 1.96 to values greater than 200 µM for the amastigote form. This study showed that thiazole compounds can be used as future antiparasitic agents. regions Thus 44chlorophenylthiazole chlorophenylthiazole 4 chlorophenyl properties availability activity toxicity IC IC5 1986 19 86 19.8 20 10 T 167 1 67 1.6 196 96 1.9 agents 198 8 19. 2 16 6 1. 9

Abstract In this work, an in silico study and evaluation of the cytotoxicity of 4-(4-chlorophenyl)thiazole compounds against mouse splenocytes and the chloroquine-sensitive Plasmodium falciparum 3D7 strain are reported. The in silico results showed that the compounds have important pharmacokinetic properties for compounds with potential drug candidates. Regarding cytotoxicity assays against splenocytes, the compounds have low cytotoxicity. In addition, they were able to promote activation of these cells by increasing nitric oxide production without promoting cell death. Finally, they were able to promote cell proliferation. Regarding the in vitro anti-P. falciparum activity assays, it was observed that the compounds were able to inhibit the parasite’s growth, presenting IC50 values ranging from 0.79 to greater than 10 µM. These results are promising when compared to chloroquine. Therefore, this study showed that 4-(4-chlorophenyl)thiazole compounds are promising candidates for antimalarials. work 44chlorophenylthiazole chlorophenylthiazole 4 chlorophenyl thiazole chloroquinesensitive chloroquine sensitive D 3D reported addition death Finally proliferation antiP. antiP anti P. P anti-P parasites parasite s growth IC IC5 079 0 79 0.7 1 µM Therefore antimalarials 07 7 0.

Abstract Studies have shown that Caesalpinia pulcherrima extracts promote antioxidant, healing, immunomodulating and antiparasitic activities and its polysaccharides can be used as functional food. In this sense, this work had as objective the isolation and characterization of a polysaccharide-like pectin, extracted from the C. pulcherrima leaves and its possible applications as an antioxidant and immunomodulator agent. The molecule was characterized by high performance liquid chromatography, fourier transform infrared spectroscopy and nuclear magnetic resonance spectroscopy. Its antioxidant potential was evaluated through the methods of phosphomolybdenum, ABTS radical scavenging [2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid], DPPH (1,1-diphenyl-2-picrylhydrazyl) and nitric oxide radical. The immunostimulating effects of pectin were tested in splenocytes to evaluate its toxic, proliferative and cell activator and immunomodulatory potential. The polysaccharide obtained has structural characteristics similar to pectins. Pectin showed high in vitro antioxidant activity for ABTS radical scavenging, moderate activity for phosphomolybdenum and low activity for DPPH and nitric oxide. In vitro immunomodulation assays showed that pectin obtained did not promote a cytotoxic effect (viability > 90%). The increase in cytosolic ROS levels indicates a possible mechanism of cell activation without causing damage. Immunophenotyping showed that pectin increased a subpopulation of CD8+ T lymphocytes and monocytes. In addition, it promoted a mostly pro-inflammatory response confirmed by the production of cytokines IL-2, -4, -6, IFN-γ and TNF-α. These results reinforce the ethnopharmacological use of C. pulcherrima leaves and expand the use of this plant for future applications as herbal medicines.

Abstract: Currently, the research of new natural compounds with biological potential demonstrates great ethnopharmacological importance. In this study, we evaluated the biological properties promoted by saline extract from Malpighia emarginata DC leaves, whose objective is to evaluate the antioxidant, antimicrobial and cytotoxicity potential. Phytochemical characterization was performed by UPLC-MS chromatography to identify the chemical compounds. For the antioxidant potential, DPPH, ATT and FRAP methods were used. The antibacterial and antifungal tests were performed evaluating the MIC50, MIC90, CMB and CMF parameters. Moreover, antibiofilm action was evaluated. Cytotoxicity and proliferation were performed using splenocytes from Balb/c mice and were evaluated by cytometry. We found a list of phenolic compounds among other bioactive compounds in the M. emarginata saline extract. In addition, higher antioxidant profile and antifungal activity against different strains of Candida spp. was promoted by the saline extract. Splenocytes showed greater cell viability (more than 90%) and showed higher proliferate index in 24 and 48 hours of incubation with the extract. Saline extract from Malpighia emarginata DC has potential action like antioxidant and antifungal agent without promote animal cell damage.