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1.
Int J Biol Macromol ; 277(Pt 4): 134644, 2024 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-39128740

RESUMO

This research describes the synthesis of a silane derivative containing phosphorus and nitrogen atoms, leveraging their synergistic flame retardant effect through the incorporation of a PH bond to the isocyanate moiety. The synthesized silane featured alkoxysilyl groups, facilitating permanent bonds with the cotton fabric surface via hydrolysis. Cotton fabrics were modified using silane solutions of varying concentrations (2.5 %, 5 %, and 10 %) through a dip-coating process to determine the effect of the modifier amount on fabric properties. The modified fabrics were subjected to FT-IR, TGA, SEM, and EDS analyses, as well as microcalorimetric and LOI tests, to assess changes in flammability. FT-IR, SEM/EDS, and add-on analyses confirmed effective coverage of the cotton fabric with the flame retardant. Thermogravimetric tests indicated a significant reduction in the mass loss rate during thermal degradation. LOI analyses demonstrated a decrease in flammability (increase in LOI value), while microcalorimetric tests showed a substantial decrease in the heat release rate, correlating with increased modifier concentration on the fabric surface. Post-washing analyses revealed that, although some of the modifier was washed out, the samples still retained reduced flammability.


Assuntos
Fibra de Algodão , Retardadores de Chama , Retardadores de Chama/síntese química , Silanos/química , Têxteis , Espectroscopia de Infravermelho com Transformada de Fourier , Termogravimetria , Organofosfonatos/química
2.
J Enzyme Inhib Med Chem ; 30(5): 767-72, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-25669348

RESUMO

Autotaxin is an extracellular, two zinc-centered enzyme that hydrolyzes lysophosphatidyl choline to lysophosphatidic acid, involved in various cancerous processes, e.g. migration, proliferation and tumor progression. We examined the autotaxin inhibitory properties of extended structure carbamoylphosphonates (CPOs) PhOC(6)H(4)SO(2)NH(CH(2))nNHCOPO(3)H(2), with increasing lengths of methylene chains, (CH(2))(n), n = 4-8. Carbamoylphosphonates having n = 6, 7, 8 inhibited autotaxin in vitro with IC(50) ≈ 1.5 µM. Using an imaging probe we demonstrated that compound n = 6 inhibits recombinant autotaxin activity in vitro and in vivo, following oral CPO administration. Additionally, daily oral administration of compound n = 7 inhibited over 90% of lung metastases in a murine melanoma metastasis model. Both the carbamoylphosphonates and the enzymes reside and interact in the extracellular space expecting minimal toxic side effects, and presenting a novel approach for inhibiting tumor proliferation and metastasis dissemination.


Assuntos
Antineoplásicos/farmacologia , Neoplasias Pulmonares/tratamento farmacológico , Melanoma Experimental/tratamento farmacológico , Organofosfonatos/farmacologia , Diester Fosfórico Hidrolases/metabolismo , Sulfonamidas/farmacologia , Administração Oral , Animais , Antineoplásicos/administração & dosagem , Antineoplásicos/química , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Humanos , Neoplasias Pulmonares/secundário , Camundongos , Camundongos Endogâmicos C57BL , Estrutura Molecular , Organofosfonatos/administração & dosagem , Organofosfonatos/química , Relação Estrutura-Atividade , Sulfonamidas/administração & dosagem , Sulfonamidas/química
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