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排序方式: 共有206条查询结果,搜索用时 312 毫秒
141.
Lalgudi S. Harikrishnan Jayakumar Warrier Andrew J. Tebben Gopikishan Tonukunuru Sudhakara R. Madduri Vishweshwaraiah Baligar Raju Mannoori Balaji Seshadri Hasibur Rahaman P.N. Arunachalam Amol G. Dikundwar Brian E. Fink Joseph Fargnoli Mark Fereshteh Yi Fan Jonathan Lippy Ching-Ping Ho Barri Wautlet Robert M. Borzilleri 《Bioorganic & medicinal chemistry》2018,26(5):1026-1034
The TGFβ-TGFβR signaling pathway has been reported to play a protective role in the later stages of tumorigenesis via increasing immunosuppressive Treg cells and facilitating the epithelial to mesenchymal transition (EMT). Therefore, inhibition of TGFβR has the potential to enhance antitumor immunity. Herein we disclose the identification and optimization of novel heterobicyclic inhibitors of TGFβRI that demonstrate potent inhibition of SMAD phosphorylation. Application of structure-based drug design to the novel pyrrolotriazine chemotype resulted in improved binding affinity (Ki apparent?=?0.14?nM), long residence time (T1/2?>?120?min) and significantly improved potency in the PSMAD cellular assay (IC50?=?24?nM). Several analogs inhibited phosphorylation of SMAD both in vitro and in vivo. Additionally, inhibition of TGFβ-stimulated phospho-SMAD was observed in primary human T cells. 相似文献
142.
Phytosynthesized silver nanoparticles as antiquorum sensing and antibiofilm agent against the nosocomial pathogen Serratia marcescens: an in vitro study 下载免费PDF全文
143.
Studies on the synthesis,characterization, human serum albumin binding and biological activity of single chain surfactant–cobalt(III) complexes 下载免费PDF全文
G. Vignesh K. Sugumar S. Arunachalam S. Vignesh R. Arthur James R. Arun K. Premkumar 《Luminescence》2016,31(2):523-532
The interaction of surfactant–cobalt(III) complexes [Co(bpy)(dien)TA](ClO4)3 · 3H2O (1) and [Co(dien)(phen)TA](ClO4)3 · 4H2O (2), where bpy = 2,2′‐bipyridine, dien = diethylenetriamine, phen = 1,10‐phenanthroline and TA = tetradecylamine with human serum albumin (HSA) under physiological conditions was analyzed using steady state, synchronous, 3D fluorescence, UV/visabsorption and circular dichroism spectroscopic techniques. The results show that these complexes cause the fluorescence quenching of HSA through a static mechanism. The binding constant (Kb) and number of binding‐sites (n) were obtained at different temperatures. The corresponding thermodynamic parameters (?G°, ?H° and ?S°) and Ea were also obtained. According to Förster's non‐radiation energy transfer theory, the binding distance (r) between the complexes and HSA were calculated. The results of synchronous and 3D fluorescence spectroscopy indicate that the binding process has changed considerably the polarity around the fluorophores, along with changes in the conformation of the protein. The antimicrobial and anticancer activities of the complexes were tested and the results show that the complexes have good activities against pathogenic microorganisms and cancer cells. Copyright © 2015 John Wiley & Sons, Ltd. 相似文献
144.
Impact of azadirachtin, an insecticidal allelochemical from neem on soil microflora, enzyme and respiratory activities 总被引:3,自引:0,他引:3
The effect of 10% azadirachtin granules (alcoholic extract of neem seed kernel mixed with China clay) was studied on the population of bacteria, actinomycetes, fungi, Azotobacter and nitrifying bacteria; soil dehydrogenase, phosphatase and respiratory activities on 0, 15th, 30th, 60th and 90th days after application in sandy loam soil collected from the fields. It was observed that baring the Azotobacter sp., azadirachtin at all the doses exerted a suppressive effect on the rest of the microbial communities and enzyme activities in the initial 15 day period. The population of bacteria, actinomycetes besides phosphatase and respiratory activities recovered after 60th day and subsequently increased significantly. The fungi and nitrifiers were most sensitive groups as their numbers were reduced significantly throughout the studies. The two times and five times recommended dose of azadirachtin had very high biocidal effects on the soil microorganisms and its activities. However, analysis of the data by the Shannon Weaver index showed that azadirachtin reduces both the form and functional microbial diversity at all doses. 相似文献
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147.
Jagadeesan Lakshmipraba Sankaralingam Arunachalam Devadas A. Gandi Thyagarajan Thirunalasundari Sivanandham Vignesh Rathinam A. James 《Luminescence》2017,32(3):309-316
Ultraviolet–visible, emission and circular dichroism spectroscopic methods were used in transfer RNA (tRNA) interaction studies performed for polyethyleneimine–copper(II) complexes [Cu(phen)(l ‐Tyr)BPEI]ClO4 (where phen =1,10‐phenanthroline, l ‐Tyr = l ‐tyrosine and BPEI = branched polyethyleneimine) with various degrees of coordination (x = 0.059, 0.149, 0.182) in the polymer chain. The results indicated that polyethyleneimine–copper(II) complexes bind with tRNA mostly through surface binding, although other binding modes, such as hydrogen bonding and van der Waals interactions, might also be present. Dye‐exclusion, sulforhodamine B and 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide assays of a polyethyleneimine–copper(II) complex with a higher degree of coordination against different cancer cell lines proved that the complex exhibited cytotoxic specificity and a significant cancer cell inhibition rate. Antimicrobial screening showed activity against some human pathogens. 相似文献
148.
Karunasagar D. Arunachalam J. Rashmi K. Naveena Lavanya Latha J. Maruthi Mohan P. 《World journal of microbiology & biotechnology》2003,19(3):291-295
A biosorbent prepared by alkaline extraction of Aspergillus niger biomass was evaluated for its potential to remove mercury species – inorganic (Hg2+) and methyl mercury (CH3Hg+) – from aqueous solutions. Batch experiments were carried out to determine the pH and time profile of sorption for both species in the pH range 2–7. The Hg2+ exhibited more rapid sorption and higher capacity than the CH3Hg+. Further, removal of both mercury species from spiked ground water samples was efficient and not influenced by other ions. Sorption studies with esterified biosorbent indicated loss of binding of both mercury species (>80%), which was regained when the ester groups were removed by alkaline hydrolysis, suggesting the involvement of carboxyl groups in binding. Further, no interconversion of sorbed species occurred on the biomass. The biosorbent was reusable up to six cycles without serious loss of binding capacity. Our results suggest that the biosorbent from Aspergillus niger can be used for removal of mercury and methyl mercury ions from polluted aqueous effluents. 相似文献
149.
A study was carried out to evaluate the anti-pyretic potential of the methanol extract of Mallotus peltatus (Geist) Muell. Arg. var acuminatus leaf, a folk medicine of Onge tribes of Bay Islands, on normal body temperature and yeast-induced pyrexia in Wister albino rats. The leaf extract at oral doses of 100, 200 and 300 mg kg(-1), p.o., showed significant reduction in normal body temperature and yeast-provoked elevated temperature in a dose-dependent manner and the anti-pyretic effect was comparable to that of standard anti-pyretic agent paracetamol (150 mg kg(-1), p.o.). The effect also extended up to 5 hours after the drug administration. 相似文献
150.
The synthesis of C19-androgens oxygenated at carbons 2, 3, 17 and 19 and of their deuterium or deuterium-tritium labeled analogs is described. 相似文献