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1.
Nat Protoc ; 14(10): 2972-2985, 2019 10.
Artigo em Inglês | MEDLINE | ID: mdl-31541227

RESUMO

Although Csp2-Csp2 Suzuki-Miyaura couplings (SMCs) are widely used in small-molecule synthesis, related methods that allow the incorporation of Csp3-hybridized coupling partners, particularly in an asymmetric manner, are less developed. This protocol describes catalytic asymmetric SMC reactions that provide access to enantiomerically enriched cyclic allylic products. The method couples racemic allyl halide starting materials with sp2-hybridized boronic acid derivatives and is compatible with heterocyclic coupling partners. These reactions are catalyzed by a rhodium-ligand complex and typically display very high levels of enantioselectivity (>95% enantiomeric excess (ee)). In this protocol, we detail a procedure using a dihydropyridine-derived allyl chloride for the synthesis of (-)-(S)-tert-butyl-3-(4-bromophenyl)-3,6-dihydropyridine-1(2H)-carboxylate, an intermediate in the synthesis of the anticancer drug niraparib. This procedure affords 1.17 g (86% yield) of the coupling product with 96% ee. The initial experimental setup of the reaction takes 45-50 min, and the reaction is complete within 4-5 h.


Assuntos
Ácidos Borônicos/química , Técnicas de Química Sintética/métodos , Ródio/química , Compostos Alílicos/química , Catálise , Indazóis/síntese química , Piperidinas/síntese química , Estereoisomerismo
2.
Nature ; 573(7773): 164, 2019 09.
Artigo em Inglês | MEDLINE | ID: mdl-31511688
3.
Eur J Med Chem ; 181: 111566, 2019 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-31401538

RESUMO

The worldwide increase of AIDS, an epidemic infection in constant development has an essential and still requires potent antiretroviral chemotherapeutic agents for reducing the integer of deaths caused by HIV. Thus, there is an urgent need for new anti-HIV drug candidates with increased strength, new targets, superior pharmacokinetic properties, and compact side effects. From this viewpoint, we first review present strategies of anti-HIV drug innovation and the synthesis of heterocyclic or natural compound as anti-HIV agents for facilitating the development of more influential and successful anti-HIV agents.


Assuntos
Fármacos Anti-HIV/química , Fármacos Anti-HIV/farmacologia , Infecções por HIV/tratamento farmacológico , HIV-1/efeitos dos fármacos , Fármacos Anti-HIV/síntese química , Técnicas de Química Sintética/métodos , Desenho de Drogas , Descoberta de Drogas , Humanos , Modelos Moleculares , Relação Estrutura-Atividade
4.
Eur J Med Chem ; 181: 111572, 2019 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-31404859

RESUMO

The discovery and development of multitarget-directed ligands (MTDLs) is a promising strategy to find new therapeutic solutions for neurodegenerative diseases (NDs), in particular for Alzheimer's disease (AD). Currently approved drugs for the clinical management of AD are based on a single-target strategy and focus on restoring neurotransmitter homeostasis. Finding disease-modifying therapies AD and other NDs remains an urgent unmet clinical need. The growing consensus that AD is a multifactorial disease, with several interconnected and deregulated pathological pathways, boosted an intensive research in the design of MTDLs. Due to this scientific boom, the knowledge behind the development of MTDLs remains diffuse and lacks balanced guidelines. To rationalize the large amount of data obtained in this field, we herein revise the progress made over the last 5 years on the development of MTDLs inspired by drugs approved for AD. Due to their putative therapeutic benefit in AD, MTDLs based on MAO-B inhibitors will also be discussed in this review.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Técnicas de Química Sintética , Desenho de Drogas , Descoberta de Drogas , Animais , Técnicas de Química Sintética/métodos , Donepezila/análogos & derivados , Donepezila/síntese química , Donepezila/farmacologia , Dopaminérgicos/síntese química , Dopaminérgicos/química , Dopaminérgicos/farmacologia , Descoberta de Drogas/métodos , Humanos , Indanos/síntese química , Indanos/química , Indanos/farmacologia , Memantina/análogos & derivados , Memantina/síntese química , Memantina/farmacologia , Terapia de Alvo Molecular , Fármacos Neuroprotetores/síntese química , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/farmacologia , Nootrópicos/síntese química , Nootrópicos/química , Nootrópicos/farmacologia , Rivastigmina/análogos & derivados , Rivastigmina/síntese química , Rivastigmina/farmacologia , Tacrina/análogos & derivados , Tacrina/síntese química , Tacrina/farmacologia
5.
Radiat Res ; 192(2): 219-230, 2019 08.
Artigo em Inglês | MEDLINE | ID: mdl-31246533

RESUMO

Primary amines form a key component of a well-studied mechanism for capturing carbon dioxide (CO2) from the atmosphere. This study comprises a single-step synthesis of a novel sorbent for CO2 by grafting monomers rich in primary amines to three commercial-grade fabrics: polyethylene terephthalate, high-density polyethylene and nylon 6. An initial evaluation of the sorbency of the chosen monomers, allylamine and butenylamine, qualitatively confirmed their ability to extract CO2 from the atmosphere. Six novel copolymers, comprised of each of the three fabrics grafted with one of each monomer, were synthesized using radiation-induced graft copolymerization through electron beam irradiation. All fabrics achieved greater grafting with butenylamine compared to allylamine, likely given the closer proximity of the primary amine to the radical on the latter's structure. Primary amines can stabilize radicals, preventing copolymerization reactions. Characterization of sorbency revealed that the majority of the grafted amines likely reacted to adsorb CO2. Therefore, the amount of amine grafted comprises the primary limiting factor on the sorbents' CO2 capacity.


Assuntos
Atmosfera/química , Dióxido de Carbono/química , Polimerização , Têxteis , Adsorção , Aminas/química , Técnicas de Química Sintética , Radioquímica
6.
Artif Cells Nanomed Biotechnol ; 47(1): 2171-2178, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31159596

RESUMO

Nanomedicine is a rapidly emerging field and is reported to be a promising tool for treating various diseases. Green synthesized nanoparticles are documented to possess a potent anticancer effect. Rabdosia rubescens is a Chinese plant which is also one of the components of PC-SPES and used to treat prostate cancer. In the present study, we synthesized the gold nanoparticles from R. rubescens (RR-AuNP) and analyzed its anticancer activity against the lung carcinoma A549 cell lines. Since lung cancer is reported to be with increased morbidity and decreased survival rate. The biosynthesized RR-AuNP were confirmed using UV-Visible spectrophotometer, size and shape of RR-AuNP were assessed by DLS, TEM and EDX. The biomolecules present in RR-AuNP and its topographical structure were detected using FTIR, SAED and AFM analysis. MTT assay was performed to detect the IC50 dose of RR-AuNP and its apoptotic effect was assessed by detecting the caspases activation, ROS generation. The anticancer effect of RR-AuNP was confirmed by DAPI staining, TUNEL assay and its molecular mechanism were confirmed by assessing the apoptotic signalling molecules protein expression. Our results illustrate that RR-AuNP showed a strong absorption peak at 550 nm and the RRAuNP were polydispersed nanospheres with size of 130 nm. RR-AuNP IC50 dose against A549 lung carcinoma cell line was detected to be at 25 µg/ml. The results of DAPI staining, TUNEL and immunoblotting analysis confirms both the 25 µg/ml and 50 µg/ml of RR-AuNP possess potent anticancer and apoptotic effect, suggesting that RR-AuNP that it may be a persuasive molecule to treat lung cancer.


Assuntos
Ouro/química , Ouro/farmacologia , Isodon/química , Neoplasias Pulmonares/patologia , Nanopartículas Metálicas/química , Extratos Vegetais/química , Células A549 , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Caspases/metabolismo , Técnicas de Química Sintética , Relação Dose-Resposta a Droga , Ativação Enzimática/efeitos dos fármacos , Química Verde , Humanos , Folhas de Planta/química , Espécies Reativas de Oxigênio/metabolismo , Transdução de Sinais/efeitos dos fármacos
7.
Carbohydr Res ; 480: 61-66, 2019 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-31176191

RESUMO

Herein we describe the synthesis of imidazo[2,1-b][1,3,4]thiadiazoles from carbohydrates with D-ribo and D-xylo configuration. The antiviral activity of these compounds was tested against Junín virus (the etiological agent of Argentine hemorrhagic fever). The p-chlorophenyl derivatives showed antiviral activity in a range of micromolar concentration.


Assuntos
Antivirais/síntese química , Antivirais/farmacologia , Ribose/química , Tiadiazóis/síntese química , Tiadiazóis/farmacologia , Xilose/química , Antivirais/química , Técnicas de Química Sintética , Vírus Junin/efeitos dos fármacos , Tiadiazóis/química
8.
Carbohydr Res ; 480: 67-72, 2019 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-31176192

RESUMO

An improved process for chemical synthesis of l-fructose with high purity in large scale from readily available l-sorbose is described. In general, this synthetic scheme is characterized by inexpensive and easily available starting materials, simple and safe experimental procedures, short time period, low environmental impact, and great potential for scaling up. The scale-up experiment (100 g) was carried out to provide 42.7 g of l-fructose with high HPLC purity of 99.65% in total yield of 50.2%. Consequently, the described improvements would be helpful for those who may wish to use l-fructose and promoting the further evaluation of applications of l-fructose.


Assuntos
Frutose/química , Frutose/síntese química , Configuração de Carboidratos , Técnicas de Química Sintética , Cinética , Modelos Moleculares , Estereoisomerismo
9.
Molecules ; 24(11)2019 May 29.
Artigo em Inglês | MEDLINE | ID: mdl-31146429

RESUMO

A concise synthetic route from methylmalonate to a tetravalent aliphatic scaffold has been developed. The ensuing tetra-tethered derivative is equipped with two hydroxyl groups, as well as orthogonal alkene and alkyne functionalities. The usefulness of the scaffold has been demonstrated with the preparation of two representative multivalent derivatives: (i) a tetravalent compound containing two D-mannose units, one fluorescent boron-dipyrromethene (BODIPY) dye and a suitably functionalized amino acid and (ii) by way of dimerization and saponification, a water-soluble tetramannan derivative containing two fluorescent BODIPY units. Additionally, photophysical measurements conducted on these derivatives support the viability of the herein designed single and double BODIPY-labeled carbohydrate-based clusters as fluorescent markers.


Assuntos
Compostos de Boro/química , Carboidratos/química , Malonatos/química , Técnicas de Química Sintética , Estrutura Molecular , Análise Espectral
10.
Molecules ; 24(11)2019 May 29.
Artigo em Inglês | MEDLINE | ID: mdl-31146470

RESUMO

Microbial resistance to drugs is an unresolved global concern, which is present in every country. Developing new antibiotics is one of the guidelines of the Centers for Disease Control and Preventions (CDC) to combat bacterial resistance to drugs. Based on our lead molecules, we report the synthesis and antimicrobial studies of 27 new pyrazole derivatives. These new coumarin-pyrazole-hydrazone hybrids are readily synthesized from commercially available starting materials and reagents using benign reaction conditions. All the synthesized molecules were tested against 14 Gram-positive and Gram-negative bacterial strains. Several of these molecules have been found to be potent growth inhibitors of several strains of these tested bacteria with minimum inhibitory concentrations as low as 1.56 µg/mL. Furthermore, active molecules are non-toxic in in vitro and in vivo toxicity studies.


Assuntos
Acinetobacter baumannii/efeitos dos fármacos , Antibacterianos/síntese química , Antibacterianos/farmacologia , Farmacorresistência Bacteriana/efeitos dos fármacos , Hidrazonas/síntese química , Hidrazonas/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Acinetobacter baumannii/metabolismo , Animais , Antibacterianos/química , Técnicas de Química Sintética , Humanos , Hidrazonas/química , Camundongos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Staphylococcus aureus/metabolismo
11.
Molecules ; 24(11)2019 May 29.
Artigo em Inglês | MEDLINE | ID: mdl-31146483

RESUMO

A series of 16-(α-alkoxyalkane)-17-hydrazino-estra-1(10),2,4-trien[17,16-c]-3-ol (3a-l) and estra-1(10),2,4-trien-[17,16-c]pyrazoline-3-ol derivatives (4a-d) were synthesized from corresponding arylidines 2a,b which was prepared from estrone 1 as starting material. Condensation of 1 with aldehydes gave the corresponding arylidine derivatives 2a,b which were treated with hydrazine derivatives in alcohols to give the corresponding derivatives 3a-l, respectively. Additionally, treatment of 2a,b with methyl- or phenylhydrazine in ethanolic potassium hydroxide afforded the corresponding N-substituted pyrazoline derivatives 4a-d, respectively. All these derivatives showed potent anti-ovarian cancer both in vitro and in vivo. The mechanism of anti-ovarian cancer was suggested to process via topoisomerase II and V600EBRAF inhibition.


Assuntos
Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Estrona/química , Inibidores de Proteínas Quinases/síntese química , Inibidores de Proteínas Quinases/farmacologia , Inibidores da Topoisomerase II/síntese química , Inibidores da Topoisomerase II/farmacologia , Animais , Antineoplásicos/química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Técnicas de Química Sintética , Modelos Animais de Doenças , Estrona/análogos & derivados , Feminino , Humanos , Camundongos , Inibidores de Proteínas Quinases/química , Proteínas Proto-Oncogênicas B-raf/antagonistas & inibidores , Inibidores da Topoisomerase II/química , Ensaios Antitumorais Modelo de Xenoenxerto
12.
Molecules ; 24(11)2019 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-31151176

RESUMO

Oxidative stress has been incriminated in the physiopathology of many diseases, such as diabetes, cancer, atherosclerosis, and cardiovascular and neurodegenerative diseases. There is a great interest in developing new antioxidants that could be useful for preventing and treating conditions for which oxidative stress is suggested as the root cause. The thiazolidine-2,4-dione derivatives have been reported to possess various pharmacological activities and the phenol moiety is known as a pharmacophore in many naturally occurring and synthetic antioxidants. Twelve new phenolic derivatives of thiazolidine-2,4-dione were synthesized and physicochemically characterized. The antioxidant capacity of the synthesized compounds was assessed through several in vitro antiradical, electron transfer, and Fe2+ chelation assays. The top polyphenolic compounds 5f and 5l acted as potent antiradical and electron donors, with activity comparable to the reference antioxidants used. The ferrous ion chelation capacity of the newly synthesized compounds was modest. Several quantum descriptors were calculated in order to evaluate their influence on the antioxidant and antiradical properties of the compounds and the chemoselectivity of the radical generation reactions has been evaluated. The correlation with the energetic level of the frontier orbitals partially explained the antioxidant activity, whereas a better correlation was found while evaluating the O-H bond dissociation energy of the phenolic groups.


Assuntos
Antioxidantes/química , Antioxidantes/farmacologia , Depuradores de Radicais Livres/química , Depuradores de Radicais Livres/farmacologia , Tiazolidinedionas/química , Tiazolidinedionas/farmacologia , Antioxidantes/síntese química , Quelantes/síntese química , Quelantes/química , Quelantes/farmacologia , Técnicas de Química Sintética , Transporte de Elétrons , Depuradores de Radicais Livres/síntese química , Radicais Livres/antagonistas & inibidores , Humanos , Estrutura Molecular , Fenóis/química , Teoria Quântica , Tiazolidinedionas/síntese química
13.
Molecules ; 24(11)2019 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-31151186

RESUMO

Two 2,3-disubstituted benzofurans (1 and 2), analogs of gamma-aminobutyric acid (GABA), were synthesized to obtain their 2,3-dihydro derivatives from the Pd/C-driven catalytic reduction of the double bond in the furanoid ring. The synthesis produced surprising by-products. Therefore, theoretical calculations of global and local reactivity were performed based on Pearson's hard and soft acids and bases (HSAB) principle to understand the regioselectivity that occurred in the reduction of the olefinic carbons of the compounds. Local electrophilicity (ωk) was the most useful parameter for explaining the selectivity of the polar reactions. This local parameter was defined with the condensed Fukui function and redefined with the electrophilic (Pk+) Parr function. The similar patterns of both resulting sets of values helped to demonstrate the electrophilic behavior (soft acid) of the olefinic carbons in these compounds. The theoretical calculations, nuclear magnetic resonance, and resonance hybrids showed the moieties in each compound that are most susceptible to reduction.


Assuntos
Benzofuranos/química , Modelos Químicos , Oxirredução , Teoria Quântica , Benzofuranos/síntese química , Catálise , Técnicas de Química Sintética , Espectroscopia de Ressonância Magnética , Estrutura Molecular
14.
Molecules ; 24(11)2019 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-31151219

RESUMO

A series of oxime Cyclohexyl (E)-4-(hydroxyimino)-4-phenylbutanoates and their ethers were designed, synthesized, and evaluated for anti-hepatitis B virus (HBV) activities with HepG 2.2.15 cell line in vitro. Most of these compounds possessed anti-HBV activities, and among them, compound 4B-2 showed significant inhibiting effects on the secretion of HBsAg (IC50 = 63.85 ± 6.26 µM, SI = 13.41) and HBeAg (IC50 = 49.39 ± 4.17 µM, SI = 17.34) comparing to lamivudine (3TC) in HBsAg (IC50 = 234.2 ± 17.17 µM, SI = 2.2) and HBeAg (IC50 = 249.9 ± 21.51 µM, SI = 2.07). Docking study of these compounds binding to a protein residue (PDB ID: 3OX8) from HLA-A2 that with the immunodominant HBcAg18-27 epitope (HLA-A2.1- restricted CTL epitope) active site was carried out by using molecular operation environment (MOE) software. Docking results showed that behaviors of these compounds binding to the active site in HLA-A protein residue partly coincided with their behaviors in vitro anti-HBV active screening.


Assuntos
Antivirais/química , Antivirais/farmacologia , Técnicas de Química Sintética , Desenho de Drogas , Vírus da Hepatite B/efeitos dos fármacos , Antivirais/síntese química , Sítios de Ligação , Domínio Catalítico , Relação Dose-Resposta a Droga , Humanos , Concentração Inibidora 50 , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Oximas/síntese química , Oximas/química , Oximas/farmacologia , Ligação Proteica , Relação Estrutura-Atividade , Replicação Viral/efeitos dos fármacos
15.
Molecules ; 24(11)2019 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-31151235

RESUMO

Background: Acridine and thiourea derivatives are important compounds in medicinal chemistry due to their diverse biological properties including anticancer and antimicrobial effects. However, literature reveals some side effects associated with use of acridines. It is suggested that hybrid molecules may reduce the side effects and enhance the beneficial properties due to synergistic activity. The objectives of the present study are to synthesize and evaluate the anticancer and antimicrobial properties of new hybrids of acridine thiosemicarbazides derivatives. Results: The structures of the synthesized compounds 4a-4e were elucidated by MS and NMR spectra. In antimicrobial assay, Compound 4c exhibited potent antimicrobial activity compared to the other four compounds. In anticancer studies, we observed that compounds 4a, 4b, 4d and 4e exhibited high cytotoxicity against the MT-4 cell line, with IC50 values of 18.42 ± 1.18, 15.73 ± 0.90, 10.96 ± 0.62 and 11.63 ± 0.11 µM, respectively. The evaluation of anticancer effects, and the associated mechanism reveals that, the anticancer activities may be related to Topo I inhibitory activity, apoptosis and cell-cycle. Molecular docking studies revealed that the presence of planar naphtho-fused rings and a flexible thiourea group together, could improve DNA-intercalation and inhibition of DNA-Topo I activity. Conclusions: The results of this study demonstrate that the rational design of target derivatives as novel antimicrobial or antitumor leads is feasible.


Assuntos
Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Desenho de Drogas , Semicarbazidas/química , Semicarbazidas/farmacologia , Anti-Infecciosos/síntese química , Antineoplásicos/síntese química , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Técnicas de Química Sintética , Humanos , Concentração Inibidora 50 , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Estrutura Molecular , Semicarbazidas/síntese química , Análise Espectral
16.
Molecules ; 24(11)2019 May 31.
Artigo em Inglês | MEDLINE | ID: mdl-31159274

RESUMO

Tetrahydropyran (THP) rings are common in several natural products, therefore, various strategies are being developed to synthesize these rings. The present work described the study of a one-pot synthesis of 2,4,6-trisubstituted tetrahydropyran compounds promoted by the ionic liquid 1-butyl-3-methylimidazolium hexafluorophosphate [BMIM][PF6] through a Barbier-Prins reaction between allyl bromide and aldehydes. The use of [BMIM][PF6] gave Prins products from several aldehydes in good yields and reaction times. We also found that the anion, PF6-, accelerates the Barbier reaction when used alone, and the excess SnBr2 from the reaction conditions of the Barbier reaction leads to the formation of the THP rings, thus acting as a catalyst for Prins cyclization. Additionally, we demonstrate that ionic liquid can be recovered and reused five times in the preparation of 4-bromo-tetrahydro-2,6-diphenyl-2H-pyran without significant yield loss.


Assuntos
Alcaloides de Berberina/síntese química , Imidazóis/química , Líquidos Iônicos/química , Catálise , Técnicas de Química Sintética , Estrutura Molecular
17.
Molecules ; 24(11)2019 May 31.
Artigo em Inglês | MEDLINE | ID: mdl-31159301

RESUMO

An efficient and practical method was developed for the synthesis of new (1,2,3triazol4yl)methyl phosphinates and (1,2,3-triazol-4-yl)methyl phosphates by the copper(I)catalyzed azide-alkyne cycloaddition (CuAAC) of organic azides and prop-2-ynyl phosphinate or prop-2-ynyl phosphate. The synthesis of (1benzyl-1H-1,2,3-triazol-4-yl)methyl diphenylphosphinate was optimized with respect to the reaction parameters, such as the temperature, reaction time, and catalyst loading. The approach was applied to a range of organic azides, which confirmed the wide scope and the substituent tolerance of the process. The method elaborated represents a novel approach for the synthesis of the target compounds.


Assuntos
Alquinos/química , Azidas/química , Cobre/química , Reação de Cicloadição , Fosfatos/síntese química , Triazóis/química , Técnicas de Química Sintética , Química Click , Espectroscopia de Ressonância Magnética , Fosfatos/química
18.
Molecules ; 24(11)2019 Jun 04.
Artigo em Inglês | MEDLINE | ID: mdl-31167363

RESUMO

To discover new antiproliferative agents with high efficacy and selectivity, a new series of 1-aryl-3-{4-[(pyridin-2-ylmethyl)thio]phenyl}urea derivatives (7a-7t) were designed, synthesized and evaluated for their antiproliferative activity against A549, HCT-116 and PC-3 cancer cell lines in vitro. Most of the target compounds demonstrated significant antiproliferative effects on all the selective cancer cell lines. Among them, the target compound, 1-[4-chloro-3-(trifluoromethyl)phenyl]-3-{4-{{[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methyl}thio}phenyl}urea (7i) was identified to be the most active one against three cell lines, which was more potent than the positive control with an IC50 value of 1.53 ± 0.46, 1.11 ± 0.34 and 1.98 ± 1.27 µM, respectively. Further cellular mechanism studies confirmed that compound 7i could induce the apoptosis of A549 cells in a concentration-dependent manner and elucidated compound 7i arrests cell cycle at G1 phase by flow cytometry analysis. Herein, the studies suggested that the 1-aryl-3-{4-[(pyridin-2-ylmethyl)thio]phenyl}urea skeleton might be regarded as new chemotypes for designing effective antiproliferative agents.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Desenho de Drogas , Compostos de Fenilureia/química , Compostos de Fenilureia/farmacologia , Antineoplásicos/síntese química , Apoptose/efeitos dos fármacos , Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Técnicas de Química Sintética , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Ligações de Hidrogênio , Estrutura Molecular , Compostos de Fenilureia/síntese química , Análise Espectral , Relação Estrutura-Atividade
19.
Top Curr Chem (Cham) ; 377(3): 13, 2019 May 03.
Artigo em Inglês | MEDLINE | ID: mdl-31054016

RESUMO

Graphene-based carbocatalysts owing to numerous amazing properties such as large specific surface area, high intrinsic mobility, excellent thermal and electrical conductivities, chemical stability, ease of functionalization, simple method of preparation, effortless recovery and recyclability have gained a superior position amongst the conventional homogeneous and heterogeneous catalysts. In this review, an endeavor has been made to highlight the syntheses of diverse heterocyclic compounds catalyzed by graphene-based catalysts. Further, the study also reveals that all the catalysts could be reused several times without significant loss in their catalytic activity. Additionally, most of the reactions catalyzed by graphene-based carbocatalysts were carried out at ambient temperature and under solvent-free conditions. Thus, the graphene-based catalysts do not merely act as efficient catalysts but also serve as sustainable, green catalysts. This review is divided into various sub-sections, each of which comprehensively describes the preparation of a particular heterocyclic scaffold catalyzed by graphene-derived carbocatalyst in addition to synthesis of graphene oxide and reduced graphene oxide, functionalization, and structural features governing their catalytic properties. Synthesis of heterocycles catalyzed by graphene-based carbocatalysts.


Assuntos
Técnicas de Química Sintética/métodos , Grafite/química , Compostos Heterocíclicos/síntese química , Catálise , Compostos Heterocíclicos/química
20.
Ultrason Sonochem ; 56: 134-142, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31101247

RESUMO

Herein, we have reported a simple sonochemical synthesis of multi-layer graphene covered tungsten trioxide nanoballs (WO3 NBs) and the nanocomposite was characterized by FESEM, HRTEM, XRD, XPS, CV and EIS. Furthermore, progesterone (PGT) is a preferred marker for various biological problems like pregnancy problem, mood swings, anxiety, depression, nervousness and body pain. Therefore, its selective and sensitive determination in various biological fluids is beneficial for the evaluation of malformation problems. We describe the fabrication of an amperometric and non-enzymatic biosensor based on WO3 NBs@GR nanocomposite modified electrode for nanomolar detection of PGT. The results showed that the nanocomposite modified electrode exhibit well-defined electro-oxidation peak compared to bare and control electrodes, demonstrating the superior electrocatalytic ability and performances. The fabricated modified sensor was facilitates the analysis of PGT in the concentration ranges of 0.025-1792.5 µM with a low detection limit of 4.28 nM. Further, the as-prepared WO3 NBs@GR electrode has been applied to determination of PGT in human blood samples with outstanding recovery results and more importantly, the facile and environment-friendly sonochemical construction strategy extended here, may be open a cost-effective way for setting up the nanocomposites based (bio) sensing platform.


Assuntos
Eletroquímica/instrumentação , Grafite/química , Limite de Detecção , Óxidos/química , Tungstênio/química , Ondas Ultrassônicas , Catálise , Técnicas de Química Sintética , Eletrodos , Oxirredução , Propriedades de Superfície , Temperatura Ambiente
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