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排序方式: 共有335条查询结果,搜索用时 312 毫秒
141.
Varaprasad CV Barawkar D El Abdellaoui H Chakravarty S Allan M Chen H Zhang W Wu JZ Tam R Hamatake R Lang S Hong Z 《Bioorganic & medicinal chemistry letters》2006,16(15):3975-3980
3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles were discovered as potent in vitro MEK1 inhibitors. 相似文献
142.
Saha S Majumdar R Dighe RR Chakravarty AR 《Metallomics : integrated biometal science》2010,2(11):754-765
Ternary cobalt(III) complexes [CoL(B)] (1-3) of a trianionic tetradentate phenolate-based ligand (L) and phenanthroline bases (B), viz. 1,10-phenanthroline (phen in 1), dipyridoquinoxaline (dpq in 2) and dipyridophenazine (dppz in 3) are synthesized, characterized from X-ray crystallographic, analytical and spectral techniques, and their utility in photodynamic therapy (PDT) of thyroid diseases caused by TSH receptor dysfunction is probed. The complexes display a visible spectral band within the PDT spectral window at ~690 nm. Photodynamic potential was estimated through DNA cleavage activity of the dpq and dppz complexes in UV-A light of 365 nm and red light of 676 nm. The reactions proceed via the hydroxyl radical pathway. The complexes retain their DNA photocleavage activity in red light under anaerobic conditions, a situation normally prevails in hypoxic tumor core. Investigation into the photocytotoxic potential of these complexes showed that the dppz complex 3 is approximately 4-fold more active in the HEK293 cells expressing human thyrotropin receptor (HEK293-hTSHR) than in the parental cell line and has an insignificant effect on an unrelated human cervical carcinoma cell line (HeLa). Photoexcitation of complex 3 in HEK293-hTSHR cells leads to damage hTSHR as evidenced from the decrease in cAMP formation both in absence and presence of hTSH and decrease in the TSHR immunofluorescence with a concomitant cytoplasmic translocation of the membrane protein, cadherin. The involvement of hTSHR is evidenced from the ability of complex 3 to bind to the extracellular domain of hTSHR (hTSHR-ECD) with a K(d) value of 81 nM and from the photocleavage of hTSHR-ECD. 相似文献
143.
Sriram Tyagarajan Prasun K. Chakravarty Bishan Zhou Michael H. Fisher Mathew J. Wyvratt Kathy Lyons Tracy Klatt Xiaohua Li Sanjeev Kumar Brande Williams John Felix Birgit T. Priest Richard M. Brochu Vivien Warren McHardy Smith Maria Garcia Gregory J. Kaczorowski William J. Martin Catherine Abbadie Erin McGowan William H. Parsons 《Bioorganic & medicinal chemistry letters》2010,20(18):5536-5540
Voltage-gated sodium channels have been shown to play a critical role in neuropathic pain. With a goal to develop potent peripherally active sodium channel blockers, a series of low molecular weight biaryl substituted imidazoles, oxazoles, and thiazole carboxamides were identified with good in vitro and in vivo potency. 相似文献
144.
Rajdeep Chakravarty Md. Motiar R. Khan Akhil R. Das Arun K. Guha 《Engineering in Life Science》2013,13(3):312-322
The adsorption of tri‐ and hexavalent chromium by the husk of Lathyrus sativus (HLS), which is an agro‐waste has been investigated to find a potential solution to environmental pollution. The pH‐dependent adsorption process finds the optimum values for trivalent and hexavalent chromium ions at about pH 5.0 and pH 2.0, respectively. The process is very fast initially and attains an equilibrium within 90 min following pseudo second‐order rate kinetics. Equilibrium adsorption data can best elucidated by the Langmuir–Freundlich dual model (r2 = 0.998) in comparison with other isotherm models examined indicating that both physi‐ and chemisorption are components of the binding mechanism of chromium ions on HLS. The results show that one gram of HLS can adsorb 24.6 mg Cr3+ and 44.5 mg Cr6+. Fourier transform infrared data and functional group modification experiments indicate that –NH2, ‐COOH, ‐OH, ‐PO43? groups of the biomass interact chemically with the chromium ions. SEM‐energy dispersive X‐ray analysis and X‐ray diffraction spectrum analysis were used to further assess the morphological changes and the mechanisms of chromium ion interaction with HLS. The analysis signified that the biosorption process involved surface morphological changes, complexation and an ion exchange mechanism. The amorphous nature of HLS facilitating metal biosorption was indicated by the X‐ray diffraction analysis. 相似文献
145.
146.
S. Sen S. Chakravarty 《Computer methods in biomechanics and biomedical engineering》2013,16(5):523-529
The present study deals with an appropriate mathematical model of an artery in the presence of constriction in which the generated wall shear stress due to blood flow is analysed. The geometry of the stenosed arterial segment in the diseased state, causing malfunction of the cardiovascular system, is formed mathematically. The flowing blood contained in the stenosed artery is treated as non-Newtonian and the flow is considered to be two-dimensional. The motion of the arterial wall and its effect on local fluid mechanics is not ruled out from the present pursuit. The flow analysis applies the time-dependent, two-dimensional incompressible nonlinear Navier–Stokes equations for non-Newtonian fluids. The flow-field can be obtained primarily following the radial coordinate transformation, using the appropriate boundary conditions and finally adopting a suitable finite difference scheme numerically. The influences of flow unsteadiness, the arterial wall distensibility and the presence of stenosis on the flow-field and the wall shear stresses are quantified in order to indicate the susceptibility to atherosclerotic lesions and thereby to validate the applicability of the present theoretical model. 相似文献
147.
K.C. Kumara Swamy G. Gangadhararao Venu Srinivas N.N. Bhuvan Kumar E. Balaraman Manab Chakravarty 《Inorganica chimica acta》2011,372(1):374-382
Use of a simple inorganic ring system with the cyclodiphosph(III)azane skeleton [e.g. [(RNH)P-N(t-Bu)]2 [R = t-Bu (7), i-Pr (8)] to probe some of the intermediates proposed in phosphine mediated organic reactions is highlighted. Thus the reaction of 7-8 with the allenylphosphine oxide Ph2P(O)C(Ph)CCH2 (9) affords the phosphinimines [(RNH)P(μ-N-t-Bu)2P(N-R)-C(CH2)CH(Ph)-P(O)Ph2] [R = t-Bu (10), i-Pr (11)], while a similar reaction of 7-8 with dimethyl maleate (or dimethyl fumarate) affords the ylides [(RNH)P(μ-N-t-Bu)2P(NH-R)C(CO2Me)-CH2(CO2Me) [R = t-Bu (18), i-Pr (19)]. The implication of such reactions on phosphine mediated organic transformations including Morita-Baylis-Hillman reaction is mentioned. In a rather rare type of situation, an unusually long phosphoryl (PO) bond [1.538 (5) Å] as revealed the X-ray structure of {(R)-6,6′-(t-Bu)2-1,1′-(C10H5)2-2,2′-O2-}{P(O)(N-t-Bu)2-P(Se)} (27) is rationalized by means of crystallographic disorder in packing after comparing the data with that in the literature and {1,1′-(C10H6)2-2,2′-O2}{P(Se)(N-t-Bu)2-P(Se)} (29). X-ray structures of the new compounds 10-11, 18-19, 27 and 29 are discussed. Compound 10 crystallizes in the chiral space group Pca2(1) with (S)-chirality at the carbon center [-C(CH2)CH(Ph)-P] suggesting a case of spontaneous resolution through crystallization. 相似文献
148.
Tyagarajan S Chakravarty PK Park M Zhou B Herrington JB Ratliff K Bugianesi RM Williams B Haedo RJ Swensen AM Warren VA Smith M Garcia M Kaczorowski GJ McManus OB Lyons KA Li X Madeira M Karanam B Green M Forrest MJ Abbadie C McGowan E Mistry S Jochnowitz N Duffy JL 《Bioorganic & medicinal chemistry letters》2011,21(2):869-873
N-type calcium channels (Cav2.2) have been shown to play a critical role in pain. A series of low molecular weight 2-aryl indoles were identified as potent Cav2.2 blockers with good in vitro and in vivo potency. 相似文献
149.
150.
Gidwani K Picado A Rijal S Singh SP Roy L Volfova V Andersen EW Uranw S Ostyn B Sudarshan M Chakravarty J Volf P Sundar S Boelaert M Rogers ME 《PLoS neglected tropical diseases》2011,5(9):e1296