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1.
Sci Rep ; 14(1): 9866, 2024 04 29.
Artigo em Inglês | MEDLINE | ID: mdl-38684797

RESUMO

A series of novel chromone derivatives of (N-(4-oxo-2-(trifluoromethyl)-4H-chromen-6-yl) benzamides) were synthesized by treating 7-amino-2-(trifluoromethyl)-4H-chromen-4-one with K2CO3 and/or NaH, suitable alkyl halides and acetonitrile and/or 1,4-dioxane. The obtained products are in high yields (87 to 96%) with various substituents in short reaction times with no more by-products and confirmed by FT-IR, 1H, and 13C-NMR Spectral data. The in vitro cytotoxic activity was examined against two human cancer cell lines, namely the human lung adenocarcinoma (A-549) and the human breast (MCF-7) cancer cell line. Compound 4h showed promising cytotoxicity against both cell lines with IC50 values of 22.09 and 6.40 ± 0.26 µg/mL respectively, compared to that of the standard drug. We also performed the in vitro antioxidant activity by DPPH radical, hydrogen peroxide, NO scavenging, and total antioxidant capacity (TAC) assay methods, and they showed significant activities. The possible binding interactions of all the synthesized chromone derivatives are also investigated against selective pharmacological targets of human beings, such as HERA protein for cytotoxic activity and Peroxiredoxins (3MNG) for antioxidant activity which showed closer binding free energies than the standard drugs and evidencing the above two types of activities.


Assuntos
Antineoplásicos , Antioxidantes , Benzamidas , Simulação de Acoplamento Molecular , Humanos , Antineoplásicos/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/química , Antioxidantes/farmacologia , Antioxidantes/síntese química , Antioxidantes/química , Benzamidas/farmacologia , Benzamidas/química , Benzamidas/síntese química , Células MCF-7 , Células A549 , Cromonas/química , Cromonas/farmacologia , Cromonas/síntese química , Linhagem Celular Tumoral , Relação Estrutura-Atividade
2.
ACS Appl Mater Interfaces ; 9(34): 29147-29156, 2017 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-28786655

RESUMO

A novel polyphosphazene (PZS) microsphere@molybdenum disulfide nanoflower (MoS2) hierarchical hybrid architecture was first synthesized and applied for enhancing the mechanical performance and flame retardancy of epoxy (EP) resin via a cooperative effect. Herein, using PZS microsphere as the template, a layer of MoS2 nanoflowers were anchored to PZS spheres via a hydrothermal strategy. The well-designed PZS@MoS2 exhibits excellent fire retardancy and a reinforcing effect. The obtained PZS@MoS2 significantly enhanced the flame-retardant performance of EP composites, which can be proved by thermogravimetric and cone calorimeter results. For instance, the incorporation of 3 wt % PZS@MoS2 brought about a 41.3% maximum reduction in the peak heat-release rate and decreased by 30.3% maximum in the total heat release, accompanying the higher graphitized char layer. With regard to mechanical property, the storage modulus of EP/PZS@MoS23.0 in the glassy state was dramatically increased to 22.4 GPa in comparison with that of pure EP (11.15 GPa). It is sensible to know that the improved flame-retardant performance for EP composites is primarily assigned to a physical barrier effect of the MoS2 nanoflowers and the polyphosphazene structure has an positive impact on promoting char formation in the condensed phase.

3.
ACS Appl Mater Interfaces ; 9(27): 23027-23038, 2017 Jul 12.
Artigo em Inglês | MEDLINE | ID: mdl-28618221

RESUMO

A novel ternary nanostructure polyphosphazene nanotube (PZS)@ mesoporous silica (M-SiO2)@bimetallic phosphide (CoCuP) was facilely fabricated, using PZS as the template, where large amount of cetyltrimethylammonium bromide molecules were anchored to PZS via a similar layer-by-layer assembly strategy, and then uniform M-SiO2 shells can be formed successfully by Hyeon's coating method. Subsequently, the three-dimensional (3D) nanostructure on the basis of bimetallic phosphide (CoCuP) interconnected with PZS@M-SiO2 was synthesized via a convenient, mild hydrothermal route. It is noted that incorporating well-designed PZS@M-SiO2@CoCuP led to significant decrease on fire hazard of thermoplastic polyurethane (TPU), that is, 58.2% and 19.4% reductions in peak heat release rate and total heat release, respectively, as well as lower toxic hydrogen cyanide and carbon monoxide yield accompanied by higher graphitized char layer. In the case of TPU/PZS@M-SiO2@CoCuP system, the storage modulus at -97 °C was dramatically improved by 62.6%, and glass transition temperature was shifted to higher value, compared to those of pure TPU. The enhanced fire safety and mechanical property for TPU composites can be ascribed to tripartite cooperative effect from respective parts (CoCuP and M-SiO2) plus the PZS.

4.
Arch Pharm (Weinheim) ; 346(9): 667-76, 2013 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-23959690

RESUMO

Syntheses of a new series of biologically potent α-aminophosphonates were accomplished by one-pot Kabachnik-Fields reaction using TiO2-SiO2 as solid supported catalyst under microwave irradiation conditions. The chemical structures of all the newly synthesized compounds were confirmed by analytical and spectral (IR, 1H, 13C, 31P NMR, and mass) data. Their anticancer nature was evaluated by screening the in vitro activity on two human cancer cell lines, HeLa and SK-BR-3. Compounds 4i and 4o showed the best activity on these cancer cells even though the majority of the compounds, and particularly 4l and 4p, have good cytotoxic activity against them.


Assuntos
Antineoplásicos/farmacologia , Química Verde/métodos , Organofosfonatos/farmacologia , Adenocarcinoma/tratamento farmacológico , Adenocarcinoma/patologia , Antineoplásicos/síntese química , Antineoplásicos/química , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/patologia , Linhagem Celular Tumoral , Feminino , Células HeLa , Humanos , Organofosfonatos/síntese química , Organofosfonatos/química , Dióxido de Silício/química , Relação Estrutura-Atividade , Titânio/química
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