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Journal of Chemical Biology

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https://www.readbyqxmd.com/read/28685001/jocb-bulletin
#1
(no author information available yet)
No abstract text is available yet for this article.
July 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28685000/amphotericin-b-potentiates-the-anticancer-activity-of-doxorubicin-on-the-mcf-7-breast-cancer-cells
#2
Farzaneh Tavangar, Hamid Sepehri, Marie Saghaeian Jazi, Jahanbakhsh Asadi
Despite the improvements in cancer treatment, breast cancer still remains the second most common cause of death from cancer in women. Doxorubicin (DOXO) is widely used for cancer treatment. However, drug resistance limits the treatment outcome. Here, we investigated the toxicity of DOXO in combination with an antifungal agent amphotericin B (AmB) against the MCF-7 breast cancer cell line. The cell viability was measured using MTT assay. The apoptosis was studied by caspase-8 and caspase-9 activity measurements and DNA fragmentation was investigated by TUNEL assay...
July 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28684999/mechanism-of-action-of-selective-inhibitors-of-il-6-induced-stat3-pathway-in-head-and-neck-cancer-cell-lines
#3
Malabika Sen, Paul A Johnston, Netanya I Pollock, Kara DeGrave, Sonali C Joyce, Maria L Freilino, Yun Hua, Daniel P Camarco, David A Close, Donna M Huryn, Peter Wipf, Jennifer R Grandis
Studies indicate that elevated interleukin-6 (IL-6) levels engage IL6Rα-gp130 receptor complexes to activate signal transducer and activator of transcription 3 (STAT3) that is hyperactivated in many cancers including head and neck squamous cell carcinoma (HNSCC). Our previous HCS campaign identified several hits that selectively blocked IL-6-induced STAT3 activation. This study describes our investigation of the mechanism(s) of action of three of the four chemical series that progressed to lead activities: a triazolothiadiazine (864669), amino alcohol (856350), and an oxazole-piperazine (4248543)...
July 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28684998/bioactive-m-ii-complexes-of-amino-acid-based-n3o-donor-mixed-ligand-in-vitro-and-in-silico-dna-binding-studies
#4
T Daniel Prakash, V Violet Dhayabaran
Three novel mixed ligand M(II) complexes, namely [CoL(1)L(2)Cl2] (1), [CuL(1)L(2)Cl2] (2), and [ZnL(1)L(2)Cl2] (3), were synthesized using 1,4-naphthoquinone, L-histidine, and 1,10-phenanthroline as ligands. The ligand framework and the corresponding structural changes on complexation were ascertained based on the results of elemental analysis, conductivity measurements, magnetic behavior, FT-IR, UV-visible, (1)H NMR, (13)C NMR, ESR spectral studies, and ESI mass spectrometry. The biological action of the ligand (L) and complexes 1-3 such as DNA binding and cleaving ability were studied...
July 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28684997/synthesis-of-tert-butyl-substituted-benzamido-phenylcarbamate-derivatives-anti-inflammatory-activity-and-docking-studies
#5
Shankar Bhookya, Jalapathi Pochampally, Anil Valeru, Vianala Sunitha, Saikrishna Balabadra, Vijjulatha Manga, Karunakar Rao Kudle
A series of new tert-butyl 2-(substituted benzamido) phenylcarbamate (4a-4j) were synthesized by the condensation of tert-butyl 2-amino phenylcarbamate (3) with various substituted carboxylic acid in the presence of EDCI and HOBt as coupling reagent, obtain in excellent yields. The structures of all newly synthesized compounds were characterized spectroscopically and evaluated for in vivo anti-inflammatory activity compared to the standard drug, indomethacin, by using the carrageenan-induced rat paw edema protocol...
July 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28684996/molecular-docking-pass-analysis-bioactivity-score-prediction-synthesis-characterization-and-biological-activity-evaluation%C3%A2-of-a-functionalized-2-butanone-thiosemicarbazone-ligand-and-its-complexes
#6
Tahmeena Khan, Shalini Dixit, Rumana Ahmad, Saman Raza, Iqbal Azad, Seema Joshi, Abdul Rahman Khan
2-Butanone thiosemicarbazone ligand was prepared by condensation reaction between thiosemicarbazide and butanone. The ligand was characterized by (1)H NMR, (13)C NMR, FT-IR, mass spectrometry and UV spectroscopic studies. Docking studies were performed to study inhibitory action against topoisomerase II (Topo II) and ribonucleoside diphosphate reductase (RR) enzymes. Inhibition constants (Ki ) of the ligand were 437.87 and 327.4 μM for the two enzymes, respectively. The ligand was tested for its potential anticancer activity against two cancer cell lines MDA-MB-231 and A549 using MTT assay and was found to exhibit good activity at higher doses with an IC50 = 80 μM against human breast cancer cell line MDA-MB-231...
July 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28405242/jocb-bulletin
#7
(no author information available yet)
No abstract text is available yet for this article.
April 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28405241/design-and-synthesis-of-a-new-steroid-macrocyclic-derivative-with-biological-activity
#8
Maria López-Ramos, Lauro Figueroa-Valverde, Socorro Herrera-Meza, Marcela Rosas-Nexticapa, Francisco Díaz-Cedillo, Elodia García-Cervera, Eduardo Pool-Gómez, Regina Cahuich-Carrillo
The aims of this study were to evaluate the positive inotropic effect of a new macrocyclic derivative (compound 11) and characterize the molecular mechanism involved in its biological activity. The first step was achieved by synthesis of a macrocyclic derivative involving a series of reactions for the preparation of several steroid derivatives such as (a) steroid-pyrimidinone (3 and 4), (b) steroid-amino (5), (c) steroid-imino (6), (d) ester-steroid (7 and 8), and (e) amido-steroid (9 and 10). Finally, 11 was prepared by removing the tert-butyldimethylsilane fragment of 10...
April 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28405240/targeting-the-ubiquitin-conjugating-enzyme-e2d4-for-cancer-drug-discovery-a-structure-based-approach
#9
Vishwanath Ramatenki, Ramakrishna Dumpati, Rajender Vadija, Santhiprada Vellanki, Sarita Rajender Potlapally, Rohini Rondla, Uma Vuruputuri
Cancer progression is a global burden. The incidence and mortality now reach 30 million deaths per year. Several pathways of cancer are under investigation for the discovery of effective therapeutics. The present study highlights the structural details of the ubiquitin protein 'Ubiquitin-conjugating enzyme E2D4' (UBE2D4) for the novel lead structure identification in cancer drug discovery process. The evaluation of 3D structure of UBE2D4 was carried out using homology modelling techniques. The optimized structure was validated by standard computational protocols...
April 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28101254/jocb-bulletin
#10
(no author information available yet)
No abstract text is available yet for this article.
January 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28101253/2-chromon-3-yl-imidazole-derivatives-as-potential-antimicrobial-agents-synthesis-biological-evaluation-and-molecular-docking-studies
#11
Shweta Sharma, Vishal Sharma, Gurpreet Singh, Harpreet Kaur, Shubham Srivastava, Mohan Paul S Ishar
A series of novel 2-(chromon-3-yl)-4,5-diphenyl-1H-imidazoles (4a-h) were synthesized by one pot condensation of substituted 3-formylchromones (1a-h), benzil (2) and ammonium acetate (3) in refluxing acetic acid at 110 °C under N2 atmosphere. Allylation of compounds 4a-h with allyl bromide in the presence of fused K2CO3 furnished N-allyl-2-(chromon-3-yl)-4,5-diphenyl-1H-imidazoles (6a-h). The synthesized compounds were characterized spectroscopically and evaluated for in vitro antimicrobial activity against various pathogenic bacterial and fungal strains by disc diffusion method...
January 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28101252/identification-of-proteins-from-wild-cardoon-flowers-cynara-cardunculus-l-by-a-proteomic-approach
#12
Amal Ben Amira, Julien Bauwens, Edwin De Pauw, Souhail Besbes, Hamadi Attia, Frédéric Francis, Christophe Blecker
Proteomic approach was applied to identify total proteins, particularly the enzymatic content, from wild cardoon flowers. As the selection of an appropriate sample preparation method is the key for getting reliable results, two different extraction/precipitation methods (trichloroacetic acid and phenol/ammonium acetate) were tested on fresh and lyophilized flowers. After two-dimensional electrophoresis (2D-E) separations, a better protein pattern was obtained after phenol extraction from lyophilized flowers...
January 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28101251/antifungal-and-anthelmintic-activity-of-novel-benzofuran-derivatives-containing-thiazolo-benzimidazole-nucleus-an-in-vitro-evaluation
#13
R Kenchappa, Yadav D Bodke, Sandeep Telkar, M Aruna Sindhe
A novel series of thiazolo[3,2-a]benzimidazole derivatives containing benzofuran nucleus (5a-l) have been synthesized. The key intermediate, substituted benzimidazol-sulfanyl benzofuran ethanone (3a-d) was prepared by refluxing the mixture of substituted 2-acetyl benzofuran and substituted 2-mercaptobenzimidazole in acetic acid. The cyclisation of compounds (3a-d) using polyphosphoric acid furnished the corresponding 6-substituted benzofuran thiazolo[3,2-a]benzimidazoles (4a-d). Further, the cyclized compounds (4a-d) were subjected for Mannich reaction to give corresponding Mannich bases (5a-l)...
January 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28101250/is-phosphatidylglycerol-essential-for-terrestrial-life
#14
REVIEW
Samuel Furse
Lipids are of increasing importance in understanding biological systems. Lipids carrying an anionic charge are noted in particular for their electrostatic interactions with both proteins and divalent cations. However, the biological, analytical, chemical and biophysical data of such species are rarely considered together, limiting our ability to assess the true role of such lipids in vivo. In this review, evidence from a range of studies about the lipid phosphatidylglycerol is considered. This evidence supports the conclusions that this lipid is ubiquitous in living systems and generally of low abundance but probably fundamental for terrestrial life...
January 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/27698951/jocb-bulletin
#15
(no author information available yet)
No abstract text is available yet for this article.
October 2016: Journal of Chemical Biology
https://www.readbyqxmd.com/read/27698950/the-removal-of-mercury-ii-from-water-by-ag-supported-on-nanomesoporous-silica
#16
Mohammad Ali Azizi Ganzagh, Mardali Yousefpour, Zahra Taherian
In this study, the synthesis of SBA-15/Ag nanocomposite materials with different amounts of silver (2.5, 5, and 10 %) has been investigated under acidic conditions by using P123 as a template via the direct method. The nanocomposites of SBA-15 were synthesized by the same method and by the addition of silver salt. Finally, the nanocomposite materials were examined for the removal of mercury ions from wastewater as an adsorbent by the reverse titration method. Characterization was carried out through x-ray diffraction analysis (XRD), scanning electron microscopy (SEM), transmission electron microscopy (TEM), and N2 adsorption-desorption (Brunauer-Emmett-Teller)...
October 2016: Journal of Chemical Biology
https://www.readbyqxmd.com/read/27698949/influence-of-organic-solvents-on-the-structural-and-thermal-characteristics-of-silk-protein-from-the-web-of-orthaga-exvinacea-hampson-lepidoptera-pyralidae
#17
Sajitha Narayanan, Mankadath Gokuldas
The silk protein from the web of Orthaga exvinacea was isolated, purified, and casted into films. This film was treated separately with methanol, acetone, ethyl acetate, and isopropyl alcohol in 50 % concentration for about 30 min. The treated films were thus dried in a desiccator and subjected to FTIR and TG-DTA analysis. The structural studies revealed that the organic solvents induce conformatory changes in the protein film, especially the most sensitive amide I (1650 cm(-1)) band. This band had shifted to lower wavenumber (1633-1636 cm(-1))...
October 2016: Journal of Chemical Biology
https://www.readbyqxmd.com/read/27698948/structural-insight-into-binding-mode-of-inhibitor-with-sahh-of-plasmodium-and-human-interaction-of-curcumin-with-anti-malarial-drug-targets
#18
Dev Bukhsh Singh, Seema Dwivedi
S-adenosyl-L-homocysteine hydrolase of Plasmodium falciparum (PfSAHH) is a potential drug target against malaria, and selective inhibition of PfSAHH is the excellent strategy to prevent the growth of parasite inside the host. Therefore, a comparative analysis of human S-adenosyl-L-homocysteine hydrolase (HsSAHH) and PfSAHH has been performed to explore the structural differences. Structural superimposition of PfSAHH and HsSAHH has generated the RMSD of 0.749 Å over 394 alpha carbon pairs. Residues of PfSAHH from position Tyr152 to Lys193 aligned with insertion/deletion region in HsSAHH, and these extra residues results in an extent of variation in cavity region of PfSAHH...
October 2016: Journal of Chemical Biology
https://www.readbyqxmd.com/read/27698947/synthesis-of-thiazolidine-2-4-dione-derivatives-anticancer-antimicrobial-and-dna-cleavage-studies
#19
S Vijaya Laxmi, P Anil, G Rajitha, Asha Jyothi Rao, Peter A Crooks, B Rajitha
In the search of efficient anticancer agents, here, new 5-(4-alkylbenzyledene)thiazolidine-2,4-dione derivatives (5a-g) have been successfully synthesized and characterized and are evaluated for anticancer and antimicrobial activities using DNA cleavage studies. In vitro studies on anticancer activity of compound 5d (NSC: 768619/1) was done against the full panel of 60 human tumor cell lines. The five-level dose activity results revealed that, the compound 5d was active against all the cell lines, it has shown potential activity against leukemia SR (GI50: 2...
October 2016: Journal of Chemical Biology
https://www.readbyqxmd.com/read/27493697/jocb-bulletin
#20
(no author information available yet)
No abstract text is available yet for this article.
July 2016: Journal of Chemical Biology
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