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Pesquisa : D02.522.818.222.500 [Categoria DeCS]
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[PMID]:29335211
[Au] Autor:Li PH; Jiang H; Zhang WJ; Li YL; Zhao MC; Zhou W; Zhang LY; Tang YD; Dong CZ; Huang ZS; Chen HX; Du ZY
[Ad] Endereço:Institute of Natural Medicine & Green Chemistry, School of Chemical Engineering and Light Industry, Guandong University of Technology, Guangzhou, 510006, China.
[Ti] Título:Synthesis of carbazole derivatives containing chalcone analogs as non-intercalative topoisomerase II catalytic inhibitors and apoptosis inducers.
[So] Source:Eur J Med Chem;145:498-510, 2018 Feb 10.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Novel topoisomerase II (Topo II) inhibitors have gained considerable interest for the development of anticancer agents. In this study, a series of carbazole derivatives containing chalcone analogs (CDCAs) were synthesized and investigated for their Topo II inhibition and cytotoxic activities. The results from Topo II mediated DNA relaxation assay showed that CDCAs could significantly inhibit the activity of Topo II, and the structure-activity relationship indicated the halogen substituent in phenyl ring play an important role in the activity. Further mechanism studies revealed that CDCAs function as non-intercalative Topo II catalytic inhibitors. Moreover, some CDCAs showed micromolar cytotoxic activities. The most potent compound 3h exhibited notable growth inhibition against four human cancer cell lines. Flow cytometric analysis revealed that compounds 3d and 3h arrested the HL-60 cells in sub G1 phase by induction of apoptosis. It was further confirmed by Annexin-V-FITC binding assay. Western blot analysis revealed that compound 3h induces apoptosis likely through the activation of caspase proteins.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Apoptose/efeitos dos fármacos
Carbazóis/farmacologia
Chalcona/farmacologia
DNA Topoisomerases Tipo II/metabolismo
Inibidores da Topoisomerase II/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Biocatálise
Carbazóis/síntese química
Carbazóis/química
Pontos de Checagem do Ciclo Celular/efeitos dos fármacos
Proliferação Celular/efeitos dos fármacos
Chalcona/química
Clivagem do DNA/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Células HL-60
Seres Humanos
Estrutura Molecular
Plasmídeos
Relação Estrutura-Atividade
Inibidores da Topoisomerase II/síntese química
Inibidores da Topoisomerase II/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Carbazoles); 0 (Topoisomerase II Inhibitors); 0P2197HHHN (carbazole); 5S5A2Q39HX (Chalcone); EC 5.99.1.3 (DNA Topoisomerases, Type II)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180117
[St] Status:MEDLINE


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[PMID]:28468657
[Au] Autor:Pei JP; Fan LH; Nan K; Li J; Dang XQ; Wang KZ
[Ad] Endereço:Department of Orthopaedics, the Second Affiliated Hospital of Xi'an Jiaotong University, No. 157 Xiwu Road, Xi'an, 710004, Shaanxi Province, People's Republic of China.
[Ti] Título:HSYA alleviates secondary neuronal death through attenuating oxidative stress, inflammatory response, and neural apoptosis in SD rat spinal cord compression injury.
[So] Source:J Neuroinflammation;14(1):97, 2017 May 03.
[Is] ISSN:1742-2094
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Hydroxysafflor yellow A (HSYA) is a major active component of yellow pigment extracted from safflowers; this compound possesses potent neuroprotective effects both in vitro and in vivo. However, underlying mechanism of HSYA is not fully elucidated. The present study investigated the protective effects of HSYA in rat spinal cord compression injury model and related mechanisms involved. METHODS: Sprague-Dawley rats were divided as Sham, Control, and HSYA groups (n = 30 per group). Spinal cord injury (SCI) model was induced by application of vascular clips (force of 50 g, 1 min) to the dura at T9-T10 level of vertebra. Injured animals were administered with either HSYA (8 mg/kg at 1 and 6 h after injury, then 14 mg/kg, for a total of 7 days at 24-h time intervals) or equal volume of saline by intraperitoneal injection. RESULTS: From this experiment, we discovered that SCI in rats resulted in severe trauma, which is characterized by tissue damage, lipid peroxidation, neutrophil infiltration, inflammation mediator release, and neuronal apoptosis. However, HSYA treatment significantly reduced the following: (1) degree of tissue injury (histological score) and edema; (2) neutrophil infiltration (myeloperoxidase activity); (3) oxidative stress (superoxide dismutase, malondialdehyde, and nitric oxide); (4) pro-inflammatory cytokine expression (tumor necrosis factor-α, interleukin-6, inducible nitric oxide synthase, cyclooxygenase-2); (5) nuclear factor-κB activation; (6) apoptosis (terminal deoxynucleotidyl transferase dUTP nick end labeling staining and cysteine-aspartic protease-3 activity). Moreover, in a separate set of experiments, we clearly demonstrated that HSYA treatment significantly ameliorated recovery of limb function (as evaluated by Basso, Beattie, and Bresnahan behavioral recovery scores). CONCLUSIONS: Treatment with HSYA restrains development of oxidative stress, inflammation response, and apoptotic events associated with SCI of rats, demonstrating that HSYA is a potential neuroprotectant for human SCI therapy.
[Mh] Termos MeSH primário: Apoptose/fisiologia
Chalcona/análogos & derivados
Mediadores da Inflamação/metabolismo
Neurônios/metabolismo
Estresse Oxidativo/fisiologia
Quinonas/uso terapêutico
Compressão da Medula Espinal/metabolismo
[Mh] Termos MeSH secundário: Animais
Apoptose/efeitos dos fármacos
Morte Celular/efeitos dos fármacos
Morte Celular/fisiologia
Chalcona/farmacologia
Chalcona/uso terapêutico
Mediadores da Inflamação/antagonistas & inibidores
Masculino
Neurônios/efeitos dos fármacos
Neurônios/patologia
Estresse Oxidativo/efeitos dos fármacos
Pigmentos Biológicos/farmacologia
Pigmentos Biológicos/uso terapêutico
Quinonas/farmacologia
Ratos
Ratos Sprague-Dawley
Compressão da Medula Espinal/tratamento farmacológico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Inflammation Mediators); 0 (Pigments, Biological); 0 (Quinones); 146087-19-6 (hydroxysafflor yellow A); 5S5A2Q39HX (Chalcone)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170505
[St] Status:MEDLINE
[do] DOI:10.1186/s12974-017-0870-1


  3 / 1384 MEDLINE  
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[PMID]:29288944
[Au] Autor:Park S; Kim EH; Kim J; Kim SH; Kim I
[Ad] Endereço:College of Pharmacy and Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Incheon, Republic of Korea.
[Ti] Título:Biological evaluation of indolizine-chalcone hybrids as new anticancer agents.
[So] Source:Eur J Med Chem;144:435-443, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:A new chemical space was explored based on an indolizine-chalcone hybrid, which was readily accessible by base-mediated aldol condensation of indolizine bearing a 7-acetyl group with various (hetero)aromatic aldehydes. Their anticancer effect was evaluated, revealing that indolizine-chalcone hybrids with 3,5-dimethoxyphenyl group (4h) or the halogen at the meta position (4j and 4l) could have the potential to induce the caspase-dependent apoptosis of human lymphoma cells.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Chalcona/farmacologia
Indolizinas/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Proliferação Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Chalcona/síntese química
Chalcona/química
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Indolizinas/síntese química
Indolizinas/química
Estrutura Molecular
Relação Estrutura-Atividade
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Indolizines); 274-40-8 (indolizine); 5S5A2Q39HX (Chalcone)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180223
[Lr] Data última revisão:
180223
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171231
[St] Status:MEDLINE


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[PMID]:29223717
[Au] Autor:Wang Y; Xue S; Li R; Zheng Z; Yi H; Li Z
[Ad] Endereço:Institute of Medicinal Biotechnology, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, China.
[Ti] Título:Synthesis and biological evaluation of novel synthetic chalcone derivatives as anti-tumor agents targeting Cat L and Cat K.
[So] Source:Bioorg Med Chem;26(1):8-16, 2018 01 01.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A series of chalcone derivatives bearing benzamide or benzenesulfonamide moieties were synthesized and evaluated for their anti-tumor effect on HCT116, MCF7 and 143B cell lines in vitro. SAR analysis showed that compounds bearing a benzenesulfonamide group had greater potency than those bearing a benzamide group. It was also shown that compounds with a mono-methyl or mono-halogen group at the 3-position on the terminal phenyl ring were more effective than those with trifluoromethyl or methoxy groups. Compound 8e exhibited the most potent anti-tumor activities against HCT116, MCF7 and 143B cell lines, with IC values of 0.597, 0.886 and 0.791µM, respectively. Molecular docking studies and enzymatic assays demonstrated that the anti-tumor activity of compound 8e might be regulated by Cat L and Cat K.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Catepsina K/antagonistas & inibidores
Catepsina L/antagonistas & inibidores
Chalcona/farmacologia
Inibidores de Cisteína Proteinase/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Chalcona/síntese química
Chalcona/química
Inibidores de Cisteína Proteinase/síntese química
Inibidores de Cisteína Proteinase/química
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Simulação de Acoplamento Molecular
Estrutura Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Cysteine Proteinase Inhibitors); 5S5A2Q39HX (Chalcone); EC 3.4.22.15 (CTSL1 protein, human); EC 3.4.22.15 (Cathepsin L); EC 3.4.22.38 (CTSK protein, human); EC 3.4.22.38 (Cathepsin K)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180106
[Lr] Data última revisão:
180106
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171211
[St] Status:MEDLINE


  5 / 1384 MEDLINE  
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[PMID]:29227931
[Au] Autor:Chu WC; Bai PY; Yang ZQ; Cui DY; Hua YG; Yang Y; Yang QQ; Zhang E; Qin S
[Ad] Endereço:School of Pharmaceutical Sciences, Institute of Drug Discovery and Development, Key Laboratory of Advanced Pharmaceutical Technology, Ministry of Education of China, Zhengzhou University, Zhengzhou 450001, PR China.
[Ti] Título:Synthesis and antibacterial evaluation of novel cationic chalcone derivatives possessing broad spectrum antibacterial activity.
[So] Source:Eur J Med Chem;143:905-921, 2018 Jan 01.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:There is an urgent need to identify new antibiotics with novel mechanisms that combat antibiotic resistant bacteria. Herein, a series of chalcone derivatives that mimic the essential properties of cationic antimicrobial peptides were designed and synthesized. Antibacterial activities against drug-sensitive bacteria, including Staphylococcus aureus, Enterococcus faecalis, Escherichia coli and Salmonella enterica, as well as clinical multiple drug resistant isolates of methicillin-resistant S. aureus (MRSA), KPC-2-producing and NDM-1-producing Carbapenem-resistant Enterobacteriaceae were evaluated. Representative compounds 5a (MIC: 1 µg/mL against S. aureus, 0.5 µg/mL against MRSA) and 5g (MIC: 0.5 µg/mL against S. aureus, 0.25 µg/mL against MRSA) showed good bactericidal activity against both Gram-positive and Gram-negative bacteria, including the drug-resistant species MRSA, KPC and NDM. These membrane-active antibacterial compounds were demonstrated to reduce the viable cell counts in bacterial biofilms effectively and do not induce the development of resistance in bacteria. Additionally, these representative molecules exhibited negligible toxicity toward mammalian cells at a suitable concentration. The combined results indicate that this series of cationic chalcone derivatives have potential therapeutic effects against bacterial infections.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Chalcona/farmacologia
Enterococcus faecalis/efeitos dos fármacos
Escherichia coli/efeitos dos fármacos
Salmonella enterica/efeitos dos fármacos
Staphylococcus aureus/efeitos dos fármacos
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antibacterianos/química
Cátions/síntese química
Cátions/química
Cátions/farmacologia
Chalcona/síntese química
Chalcona/química
Relação Dose-Resposta a Droga
Enterococcus faecalis/crescimento & desenvolvimento
Escherichia coli/crescimento & desenvolvimento
Testes de Sensibilidade Microbiana
Estrutura Molecular
Salmonella enterica/crescimento & desenvolvimento
Staphylococcus aureus/crescimento & desenvolvimento
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Cations); 5S5A2Q39HX (Chalcone)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180101
[Lr] Data última revisão:
180101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171212
[St] Status:MEDLINE


  6 / 1384 MEDLINE  
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[PMID]:28743509
[Au] Autor:Iftikhar S; Khan S; Bilal A; Manzoor S; Abdullah M; Emwas AH; Sioud S; Gao X; Chotana GA; Faisal A; Saleem RSZ
[Ad] Endereço:Department of Chemistry, SBASSE, Lahore University of Management Sciences, Lahore 54792, Pakistan.
[Ti] Título:Synthesis and evaluation of modified chalcone based p53 stabilizing agents.
[So] Source:Bioorg Med Chem Lett;27(17):4101-4106, 2017 09 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Tumor suppressor protein p53 induces cell cycle arrest and apoptotic cell death in response to various cellular stresses thereby preventing cancer development. Activation and stabilization of p53 through small organic molecules is, therefore, an attractive approach for the treatment of cancers retaining wild-type p53. In this context, a series of nineteen chalcones with various substitution patterns of functional groups including chloro, fluoro, methoxy, nitro, benzyloxy, 4-methyl benzyloxy was prepared using Claisen-Schmidt condensation. The compounds were characterized using NMR, HRMS, IR and melting points. Evaluation of synthesized compounds against human colorectal (HCT116) and breast (CAL-51) cancer cell lines revealed potent antiproliferative activities. Nine compounds displayed GI values in the low micromolar to submicromolar range; for example (E)-1-phenyl-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one (SSE14108) showed GI of 0.473±0.043µM against HCT116 cells. Further analysis of these compounds revealed that (E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-one (SSE14105) and (E)-3-(4-methoxyphenyl)-1-phenylprop-2-en-1-one (SSE14106) caused rapid (4 and 8-h post-treatment) accumulation of p53 in HCT116 cells similar to its induction by positive control, Nutlin-3. Such activities were absent in 3-(4-methoxyphenyl)propiophenone (SSE14106H2) demonstrating the importance of conjugated ketone for antiproliferative and p53 stabilizing activity of the chalcones. We further evaluated p53 levels in the presence of cycloheximide (CHX) and the results showed that the p53 stabilization was regulated at post-translational level through blockage of its degradation. These chalcones can, therefore, act as fragment leads for further structure optimization to obtain more potent p53 stabilizing agents with enhanced anti-proliferative activities.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Chalcona/farmacologia
Proteína Supressora de Tumor p53/metabolismo
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Chalcona/síntese química
Chalcona/química
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Células HCT116
Seres Humanos
Estrutura Molecular
Estabilidade Proteica/efeitos dos fármacos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Tumor Suppressor Protein p53); 5S5A2Q39HX (Chalcone)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170727
[St] Status:MEDLINE


  7 / 1384 MEDLINE  
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[PMID]:28869400
[Au] Autor:Singh A; Viljoen A; Kremer L; Kumar V
[Ad] Endereço:Department of Chemistry, Guru Nanak Dev University, Amritsar-143005, India.
[Ti] Título:Azide-alkyne cycloaddition en route to 4-aminoquinoline-ferrocenylchalcone conjugates: synthesis and anti-TB evaluation.
[So] Source:Future Med Chem;9(15):1701-1708, 2017 Oct.
[Is] ISSN:1756-8927
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:AIM: Tuberculosis is responsible for 9.6 million infections and 1.5 million deaths in 2015. The development of multidrug-resistant and extensively drug-resistant strains has impeded the development of effective antitubercular therapy. Results/methodology: The present manuscript describes the synthesis of a series of 4-aminoquinoline-ferrocenylchalcone conjugates via Cu-promoted Huisgen's azide-alkyne cycloaddition reaction and evaluation of their antitubercular activities against mc 6230 strain of Mycobacterium tuberculosis. The conjugate 11j proved to be the most potent of the synthesized conjugates with a minimum inhibitory concentration (MIC ) value of 30 µM and proved to be noncytotoxic against HeLa cells. CONCLUSION: The synthesized conjugates can act as starting point for the development of new antitubercular agents. Synthesis and antitubercular evaluation of 1H-1,2,3-triazole-tethered 4-aminoquinoline-ferrocenylchalcone conjugates. [Formula: see text].
[Mh] Termos MeSH primário: Aminoquinolinas/química
Antituberculosos/síntese química
Antituberculosos/farmacologia
Chalcona/síntese química
Chalcona/farmacologia
Reação de Cicloadição
[Mh] Termos MeSH secundário: Alquinos/química
Azidas/química
Sobrevivência Celular/efeitos dos fármacos
Chalcona/química
Células HeLa
Seres Humanos
Testes de Sensibilidade Microbiana
Mycobacterium tuberculosis/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkynes); 0 (Aminoquinolines); 0 (Antitubercular Agents); 0 (Azides); 5S5A2Q39HX (Chalcone); GTE5P5L97N (4-aminoquinoline)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171025
[Lr] Data última revisão:
171025
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170905
[St] Status:MEDLINE
[do] DOI:10.4155/fmc-2017-0098


  8 / 1384 MEDLINE  
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[PMID]:28838697
[Au] Autor:Rioux B; Pouget C; Fidanzi-Dugas C; Gamond A; Laurent A; Semaan J; Pinon A; Champavier Y; Léger DY; Liagre B; Duroux JL; Fagnère C; Sol V
[Ad] Endereço:Université de Limoges, Laboratoire de Chimie des Substances Naturelles, EA 1069, F-87000 Limoges, France.
[Ti] Título:Design and multi-step synthesis of chalcone-polyamine conjugates as potent antiproliferative agents.
[So] Source:Bioorg Med Chem Lett;27(18):4354-4357, 2017 09 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The aim of this study is to synthesize chalcone-polyamine conjugates in order to enhance bioavailability and selectivity of chalcone core towards cancer cells, using polyamine-based vectors. 3-hydroxy-3',4,4',5'-tetramethoxychalcone (1) and 3',4,4',5'-tetramethoxychalcone (2) were selected as parent chalcones since they were found to be efficient anti-proliferative agents on various cancer cells. A series of ten chalcone-polyamine conjugates was obtained by reacting carboxychalcones with different polyamine tails. Chalcones 1 and 2 showed a strong cytotoxic activity against two prostatic cancer (PC-3 and DU-145) and two colorectal cancer (HT-29 and HCT-116) cell lines. Then, chalcone-spermine conjugates 7d and 8d were shown to be the most active of the series and could be considered as promising compounds for colon and prostatic cancer adjuvant therapy.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Chalcona/farmacologia
Desenho de Drogas
Poliaminas/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Chalcona/química
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Estrutura Molecular
Poliaminas/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Polyamines); 5S5A2Q39HX (Chalcone)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170826
[St] Status:MEDLINE


  9 / 1384 MEDLINE  
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[PMID]:28838690
[Au] Autor:Gan X; Hu D; Chen Z; Wang Y; Song B
[Ad] Endereço:State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Research, and Development Center for Fine Chemicals, Guizhou University, Guiyang 550025, China; College of Chemistry and Li
[Ti] Título:Synthesis and antiviral evaluation of novel 1,3,4-oxadiazole/thiadiazole-chalcone conjugates.
[So] Source:Bioorg Med Chem Lett;27(18):4298-4301, 2017 09 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A series of novel 1,3,4-oxadiazole/thiadiazole-chalcone conjugates were synthesized and their in vitro and in vivo antiviral activities were evaluated via microscale thermophoresis method and half-leaf method, respectively. The in vitro results indicated that compounds 7g, 7l, 8h, and 8l displayed good antiviral activity against TMV, with the binding constant values of 5.93, 6.15, 6.02, and 5.04µM, respectively, which were comparable to that of Ninnanmycin (6.78µM) and even better than that of Ribavirin (99.25µM). The in vivo results demonstrated that compounds 7g, 7l, 8h, and 8l exhibited remarkable anti-TMV activity with the EC values of 33.66, 33.97, 33.87 and 30.57µg/mL, respectively, which were comparable to that of Ningnanmycin (36.85µg/mL) and superior to that of Ribavirin (88.52µg/mL). Interestingly, the trend of antiviral activity in vivo was consistent with the in vitro results.
[Mh] Termos MeSH primário: Antivirais/farmacologia
Chalcona/farmacologia
Oxidiazóis/farmacologia
Tiadiazóis/farmacologia
Vírus do Mosaico do Tabaco/efeitos dos fármacos
[Mh] Termos MeSH secundário: Antivirais/síntese química
Antivirais/química
Chalcona/química
Relação Dose-Resposta a Droga
Testes de Sensibilidade Microbiana
Estrutura Molecular
Oxidiazóis/química
Relação Estrutura-Atividade
Tiadiazóis/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antiviral Agents); 0 (Oxadiazoles); 0 (Thiadiazoles); 20O2F20OUR (1,3,4-oxadiazole); 5S5A2Q39HX (Chalcone)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171125
[Lr] Data última revisão:
171125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170826
[St] Status:MEDLINE


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[PMID]:28774575
[Au] Autor:Shankaraiah N; Nekkanti S; Brahma UR; Praveen Kumar N; Deshpande N; Prasanna D; Senwar KR; Jaya Lakshmi U
[Ad] Endereço:Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500 037, India. Electronic address: shankar@niperhyd.ac.in.
[Ti] Título:Synthesis of different heterocycles-linked chalcone conjugates as cytotoxic agents and tubulin polymerization inhibitors.
[So] Source:Bioorg Med Chem;25(17):4805-4816, 2017 Sep 01.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A series of new heterocycles-linked chalcone conjugates has been designed and synthesized by varying different alkane spacers. These conjugates were tested for their in vitro cytotoxic potential against a panel of selected human cancer cell lines namely, lung (A549 and NCI-H460), prostate (DU-145 and PC-3), colon (HCT-15 and HCT-116), and brain (U-87 glioblastoma) by MTT assay. Notably, among all the tested compounds, 4a exhibited potent cytotoxicity on NCI-H460 (lung cancer) cells with IC of 1.48±0.19µM. The compound 4a showed significant inhibition of tubulin polymerization and disruption of the formation of microtubules (IC of 9.66±0.06µM). Moreover, phase contrast microscopy and DAPI staining studies indicated that compound 4a can induce apoptosis in NCI-H460 cells. Further, the flow-cytometry analysis revealed that compound 4a arrests NCI-H460 cells in the G2/M phase of the cell cycle. In addition, molecular docking studies of the most active compounds 4a and 4b into the colchicine site of the tubulin, revealed the possible mode of interaction by these new conjugates.
[Mh] Termos MeSH primário: Chalcona/química
Chalcona/farmacologia
Moduladores de Tubulina/síntese química
Moduladores de Tubulina/farmacologia
[Mh] Termos MeSH secundário: Células A549
Antineoplásicos/farmacologia
Apoptose/efeitos dos fármacos
Sítios de Ligação
Linhagem Celular Tumoral
Chalcona/síntese química
Chalcona/toxicidade
Ensaios de Seleção de Medicamentos Antitumorais
Pontos de Checagem da Fase G2 do Ciclo Celular/efeitos dos fármacos
Células HCT116
Seres Humanos
Concentração Inibidora 50
Pontos de Checagem da Fase M do Ciclo Celular/efeitos dos fármacos
Potencial da Membrana Mitocondrial
Microscopia de Contraste de Fase
Simulação de Acoplamento Molecular
Estrutura Terciária de Proteína
Relação Estrutura-Atividade
Tubulina (Proteína)/química
Tubulina (Proteína)/metabolismo
Moduladores de Tubulina/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Tubulin); 0 (Tubulin Modulators); 5S5A2Q39HX (Chalcone)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170926
[Lr] Data última revisão:
170926
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170805
[St] Status:MEDLINE



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