As part of an ongoing drug development programme, this paper describes the sequence specificity and time course of DNA adduct formation for a series of novel DNA-targeted analogues of cis-diaminedichloroplatinum(II) (cisplatin) (9-aminoacridine-4-carboxamide Pt complexes) in intact HeLa cells. T...
Three platinum complexes in which substituted (7-OMe, 9-NH2; 7-F, 9-NH2; and 7-H, 9-NH(CH2)2OH) 9-aminoacridine-4-carboxamides were tethered to a platinum(II)diamine moiety were synthesised and characterised at the chemical and biological level. These variants showed a decrease in cytotoxicity, ...
We describe the synthesis of a series of DNA-threading bis(9-aminoacridine-4-carboxamides) comprising ethylpiperidino and N-methylpiperidin-4-yl sidechains, joined via neutral flexible alkyl chains, charged flexible polyamine chains and a semi-rigid charged piperazine linker. Their cytotoxicity ...
A series of intercalator-tethered platinum(II) complexes PtLCl2 have been prepared where L are the diamine ligands N-[2-[(aminoethyl)amino]ethyl]-9-aminoacridine-4-carboxamide, N-[3-[(2-aminoethyl)amino]propyl]-9-aminoacridine-4-carboxamide, N-[4-[(2-aminoethyl)amino]butyl]-9-aminoacridine-4-car...
The design of molecules that recognize the specific sequence of the DNA double helix or those that can stabilize DNA topoisomerase cleavable complex to stop the progression of DNA process, may be very useful in cancer chemotherapy. In the field of antituor DNA-intercalating agents, 9-aminoacridi...
The properties of 4H–SiC/Ni/Ti/Al/W metal contacts on n-type and p-type ion-implanted 4H–SiC layers are studied in this paper, with the aim of realizing simultaneous ohmic contact formation. The thickness of the Al film and the alloying temperature are analyzed. Specific contact resistances of...
Serotonin receptor, 5-HT1AR, agonists and partial agonists have established drug candidates for psychiatric and neurologic disorders. Recently, we reported the synthesis and evaluation of arylpiperazine derivatives of 3,5-dioxo-(2H,4H)-1,2,4-triazine as 5-HT1AR ligands. Herein, we generated a ho...
Multiple-energy He ions were used to produce thicker damage layers with 3000 appm/0.17 dpa (by low dose implantation) and 6000 appm/0.34 dpa (by high dose implantation), respectively, in mono-crystalline 4H-SiC at room temperature (RT). Results from XRD and nano-indentation tests indicated that ...
In previous works, an alternative gate oxide configuration, based on a boron treatment, was proposed in order to enhance the SiO2/SiC interface quality, enabling high channel mobility n-channel 4H-SiC lateral MOSFETs. In this paper we study the effect of this treatment on 6H-SiC MOSFETs and we c...
In this work, monolithically integrated wavelength-selective 4H-SiC UV-sensor arrays were manufactured using two photolithography masks and only one implantation sequence demonstrating the potential of the advanced 4H-SiC process technology for the first time. The process technology is described...
Thermomigration of molten Cr-Si-C alloys in silicon carbide (SiC) along a quasi-binary Cr-SiC system at 1873–2273 K was evaluated by the temperature gradient zone melting method. Solute diffusivity in the molten alloy and distribution of Cr between 4H-SiC and the alloy were studied, where both ...
Electronic structures and magnetic properties for double impurities (Fe and Cr) doped 4H silicon carbide (SiC) are studied by first principles calculations within the generalized gradient approximation (GGA) +U scheme. For single Fe-doped 4H–SiC, the local magnetic moments of Fe atom is about 3...
A 4H–SiC detector based on the Schottky diode was fabricated and the combined influence of high temperature and gamma irradiation on 4H–SiC detector has been investigated. We tested the detector's performance at high temperature before gamma irradiation. I–V characteristics and the alpha...
The synthetic utility of 3-thioxo-1,2,4-triazin-5-ones 1 and 4-amino-3-mercapto-1,2,4-triazin-5(4H)-ones 2 as building blocks for novel bis- and poly(1,2,4-triazines) via alkylation with the corresponding bis- and poly(halo) compounds was investigated. Prediction of the site of alkylation has be...
We report promising results regarding the possible use of AlN or Al2O3 as a gate dielectric in 4H-SiC MISFETs. The crystalline AlN films are grown by hot wall metal organic chemical vapor deposition (MOCVD) at 1100 °C. The amorphous Al2O3 films are grown by repeated deposition and subsequent lo...
Several analogs of 5-hydroxy-2-formylpyridine thiosemicarbazone (5-HP) that contain isosteric replacement of sulfur by Se, NH or O have been synthesized. Measurement of the antineoplastic activity of these compounds in mice bearing Sarcoma 180 ascites cells indicated that 5-HP was the most activ...
SummaryA method for the quantitative analysis of N-oxalylcysteine and oxalyl thiolesters (RSCOCOO−) in biological samples is described. These compounds were found in all rat tissues examined (kidney, liver, brain, heart, muscle and fat), with the amount of N-oxalylcysteine ranging up to 18 nmole...
A convenient method is described for the quantitative analysis of oxalyl thiolesters (OTEs), a newly discovered class of mammalian metabolites, in biological samples. By this particular technique the total concentration of all OTEs in the sample is determined. The method involves first reacting ...
According to the relationship among microbial activity, quorum sensing (QS) and structural stability of aerobic granular sludge, the mechanism of QS regulation for microbial activity and granular stability was investigated in AGS process. Results showed that ATP content decreased sharply from 1....
Quorum sensing (QS) systems, which depend on N-acylhomoserine lactone (AHL) signal molecules, mediate the production of virulence factors in many pathogenic microorganisms. One hundred and forty-six bacterial strains, isolated from a bivalve hatchery, were screened for their capacity to degrade ...
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