Cytotoxic Activity
Mostrando 1-12 de 1778 artigos, teses e dissertações.
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1. METABOLIC PROFILING AND CYTOTOXIC ACTIVITY OF METHANOL EXTRACTS FROM CHAMAECRISTA DUCKEANA (P. BEZERRA & A. FERN.) H. S. IRWIN & BARNEBY (LEGUMINOSAE, CAESALPINIOIDEAE)
The genus Chamaecrista comprises more than 330 species, with only a few studies on their chemical composition and biologic activities. In this study, the phytochemical profile of leaf, stems, and fruits extracts of the C. duckeana were examined by UPLC ESI HRMS analysis to determine possibly bioactive constituents. The antioxidant activity was carried out th
Química Nova. Publicado em: 2022
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2. Diacetate Naphthoquinone Derivatives Tethered to 1,2,3-Triazoles: Synthesis and Cytotoxicity Evaluation in Caco-2 Cells
Acetylated compounds prepared from naphthoquinones have been reported as antitumoral prodrugs. Exploring the synthetic versatility of the naphthoquinone and triazolic nuclei, herein we report a simple and efficient synthetic route to prepare a series of sixteen prodrugs prototype of 1,2,3-triazoles-naphthoquinodoic acetyl derivatives. The compounds 10a-10h a
Journal of the Brazilian Chemical Society. Publicado em: 2022
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3. Friedelane Triterpenes with Cytotoxic Activity from the Leaves of Maytenus quadrangulata (Celastraceae)
Three new triterpenes, 3,4-seco-3,11β-epoxyfriedel-4(23)-en-3β-ol (1), friedelan-3α,11β diol (2), 7β,26-epoxyfriedelan-3a,7a-diol (3), a mixture of two new triterpenes 3α-hydroxyfriedelan-29-yl palmitate (4) and 3α-hydroxyfriedelan-29-yl stearate (5) and eleven known compounds were obtained from the hexane extract of Maytenus quadrangulata leaves. The
Journal of the Brazilian Chemical Society. Publicado em: 2022
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4. CYP450 Metabolism of a Semisynthetic Naphthoquinone, an Anticancer Drug Candidate, by Human Liver Microsomes
CNFD (6b,7-dihydro-5H-cyclopenta[b]naphtho[2,1-d]furan-5,6(9aH)-dione) is a semisynthetic naphthoquinone derived from lawsone that has cytotoxic action in different tumor lines and anticancer activity in vivo. Therefore, this molecule is a relevant candidate for drug development, but there is still no information on its human metabolism and systemic eliminat
Journal of the Brazilian Chemical Society. Publicado em: 2022
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5. Promoting effects of 6-Gingerol on probiotic adhesion to colonic epithelial cells
Abstract The effects of 6-gingerol on adhesive ability of probiotics to colonic epithelial cells in vitro were explored. Two strains of probiotics were Lactophilus acidophilus and Bifidobacterium bifidum. NCM 460 cells (normal colonic epithelial cells) and Caco-2 cells (colon cancer cells) were used in this study. Effect of 6-gingerol (5, 10, 15, 20, 25, 30,
Food Sci. Technol. Publicado em: 2021-09
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6. Allyl Dibenzoylmethane Derivative: Antimelanoma Activity and Study of Its Molecular Mechanism of Interaction with DNA
In this study, we assessed the cytotoxic effect of 1,3-diphenyl-2-allyl-1,3-propanedione (DPAP) on B16F10 and Tm5 melanoma cells and investigated its interaction with DNA (deoxyribonucleic acid) using optical tweezers. The compound showed to be effective against B16F10 cells with selectivity index (SI) of 7.92 and interaction to the outer surface of the doub
J. Braz. Chem. Soc.. Publicado em: 2021-07
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7. Expedient Microwave-Assisted Synthesis of Bis(n)-lophine Analogues as Selective Butyrylcholinesterase Inhibitors: Cytotoxicity Evaluation and Molecular Modelling
In the brain of patients with chronic Alzheimer’s disease (AD), the butyrylcholinesterase (BuChE) levels rise while the acetylcholinesterase (AChE) levels decrease. Therefore, development of new selective BuChE inhibitors is of vital importance. Here we present a series of bis(n)-lophine analogues, where two lophine derivatives are connected by a methylene
J. Braz. Chem. Soc.. Publicado em: 2021-06
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8. Chemical Constituents and Cytotoxic Activity of Rhinella jimi (Anura: Bufonidae)
Rhinella jimi toads (Stevaux, 2002) belong to the Bufonidae family, are endemic in the Brazilian Northeast and are commonly found during rainy periods. In general, amphibians of this family have in their poisons different metabolites that show a diversity of pharmacological activities. The isolation and identification of these compounds are of great importan
J. Braz. Chem. Soc.. Publicado em: 2021-05
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9. Electrochemical Preparation and Evaluation of Cytotoxic Activity of Methoxyl-oxo-biseugenol, a New Oxidized Derivative of Biseugenol
Electrochemical procedures have emerged as a powerful tool for the synthesis of complex organic molecules including transformation of natural products. In this study, the electrosynthesis of biseugenol in MeOH afforded one new oxidized derivative, which was characterized as methoxyl-oxo-biseugenol (MOB) by nuclear magnetic resonance (NMR) and electrospray io
J. Braz. Chem. Soc.. Publicado em: 2021-05
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10. Design, Synthesis and Antifungal Activity of New Schiff Bases Bearing 2-Aminothiophene Derivatives Obtained by Molecular Simplification
Seventeen Schiff bases bearing 2-aminothiophene derivatives were designed and synthesized using molecular simplification. The resulting compounds (4a-4q) were evaluated for their in vitro antifungal activity against dermatophytes. Prediction of their druglikeness and pharmacokinetic properties, establishment of their structure-activity relationships (SAR), a
J. Braz. Chem. Soc.. Publicado em: 2021-05
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11. Synthesis and Biological Evaluation of Benzo[f]indole-4,9-diones N-Linked to Carbohydrate Chains as New Type of Antitumor Agents
In this work, we report the synthesis of three series of carbohydrate-based benzo[f]indole-4,9-diones and amino-1,4-naphthoquinone derivatives and evaluated their cytotoxic activity against eight human cancer cell lines. Several compounds showed a promising cytotoxic activity toward the tumor cell lines (half maximal inhibitory concentration (IC50) < 10.0 μ
J. Braz. Chem. Soc.. Publicado em: 2021-03
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12. Synthesis of 1,2,3-Triazole Benzophenone Derivatives and Evaluation of in vitro Sun Protection, Antioxidant Properties, and Antiproliferative Activity on HT-144 Melanoma Cells
Benzophenones display several biological activities, including antioxidant, anticancer, and photoprotective. Furthermore, antioxidants can minimize both ultraviolet absorption and tumor development. In the present investigation, a series of twenty-six 1,2,3-triazole-benzophenone derivatives were synthesized and had their antioxidant, anticancer, and photopro
J. Braz. Chem. Soc.. Publicado em: 2021-03