Facile Synthesis and Properties of 2‐λ5‐Phosphaquinolines and 2‐λ5‐Phosphaquinolin‐2‐ones

Treatment of 2‐ethynylanilines with P(OPh)₃ gives either 2,2‐diphenoxy‐2‐λ⁵‐phosphaquinolines or 2‐phenoxy‐2‐λ⁵‐phosphaquinolin‐2‐ones under transition‐metal‐free conditions. This reaction offers access to an underexplored heterocycle, which opens up the study of the fundamental nature of the N?P^V double bond and its potential for delocalization within a cyclic π‐electron system. This heterocycle can serve as a carbostyril mimic, with application as a bioisostere for pharmaceuticals based on the 2‐quinolinone scaffold. It also holds promise as a new fluorophore, since initial screening reveals quantum yields upwards of 40 %, Stokes shifts of 50–150 nm, and emission wavelengths of 380–540 nm. The phosphaquinolin‐2‐ones possess one of the strongest solution‐state dimerization constants for a D–A system (130 M ^?1) owing to the close proximity of a strong acceptor (P?O) and a strong donor (phosphonamidate N? H), which suggests that they might hold promise as new hydrogen‐bonding hosts for optoelectronic sensing.     

Synthesis and characterization of novel chalcones linked 3-[1-(3-chlorophenyl)-3-(pyren-1-yl)]-1H-pyrazole moiety

Russian Journal of General Chemistry - New series of pyrenyl–pyrazole based chalcones have been synthesized and characterized via the condensation of...     

Synchrotron FTIR analysis of drug treated ovarian A2780 cells: an ability to differentiate cell response to different drugs?

Recently a new di-gold(I) organometallic complex [1,3-(Ph(3)PAu)(2)-C(6)H(4)] (KF0101) has been synthesised and found to exhibit cytotoxic activity in vitro. Subsequently it has been demonstrated that KF0101 shows little or no cross-resistance against a number of the cisplatin resistant ovarian cancer cell lines in vitro suggesting a different mode of action for the drug. In this study, syncrotron radiation infrared microspectroscopy (SR-IRMS) has been used on drug treated single A2780 cells in order to determine if this different mode of action can be identified spectroscopically. The aim of the study was to establish: (i) if single cell SR-IRMS could be used to give insight into the cellular response on treatment with different cytotoxic agents relative to non-treated cells (control) and (ii) that if the cytotoxic drugs elicit a different biochemical response these responses could be distinguished from each other. The most striking features obtained after Principal Components Analysis (PCA) of Resonant Mie Scattering (RMieS) corrected single cell spectra of drug treated ovarian A2780 cells are: (i) The spectra obtained for the control are quite heterogeneous and several hundred spectra are required to adequately define the nature of the control; (ii) after drug treatment at the IC50 level for 24 h with cisplatin, KF0101, methotrexate, paclitaxel or 5-fluorouracil the cell spectra, as represented on a PCA scores plot, generally concentrate in certain well defined areas of the control, there are however a small number of spectra that fall outside of the area defined by the control; and (iii) a differentiation between cell spectra obtained on treatment with different drugs is observed which fits well with different in vitro cell culture behaviour and a flow cytometry cell cycle analysis of the control and drug treated cells. Inspection of the loading plots shows that PC1 is essentially the same for all plots and reflects changes in cell biochemistry related to the cell cycle. PC2, however, on comparison of the control versus cisplatin or cisplatin versus KF0101 is indicative of differences induced by drug treatment and has been termed as cell cycle-plus behaviour. These data are shown to be consistent with that obtained using bench-top IRMS by averaging a number of single cell spectra and carrying out a PCA, but SR-IRMS offers more insight into how the drug is affecting the cell population. More importantly, this approach enables the influence of the cell cycle on both the control and drug treated samples to be taken into consideration when evaluating the drug-cell interaction.     

Mechanism of stigmasterol dealkylation in insect

Deuterated stigmasterols (10, 11 and 12) were chemically synthesized and fed to silk-worm larvae. GC-MS analysis of the metabolites, cholesterol (4) and desmosterol (6), indicates the migration of 25-hydrogen to C-24 position during stigmasterol dealkylation. 22,24(28)-Dienes(8a and 8b) were shown to be converted to 22,24-diene (5), desmosterol and cholesterol.     

Cleavage of the N-PChd group from protected amino acids and peptides by cathodic reduction

Amino acid and peptide esters protected by the PChd group can be deprotected cathodically under mild conditions.     

Effect of some environmental ligands and fertilizers on humic acid complexation with strontium

The effect of some environmental ligands and certain fertilizers on the complexation of strontium with humic acid wasinvestigated colorimetrically and radiometrically. The results indicate that Na₂-EDTA, Na₃-citrate and NaCl compete to complex strontium in solution with the sequence: chloride < citrate < EDTA while Na₃-phosphate has the reverse behavior. In the case of nitrogen containing fertilizers, the results show that urea, Mg-ammonium nitrate and ammonium nitrate increase the availability of strontium to plants and microorganisms.     

Solochrome Violett R. S. as a new colorimetric reagent

Summary The reaction between molybdenum and the sulphonic acid azo dye Solochrome Violet R.S. has proved to be a suitable one for the microdetermination of Mo amounts covering the range of 0.3 to 10 ppm in purely aqueous solutions. The variation of extinction with concentration conforms satisfactorily with Beer's law throughout the whole range. Very many cations and anions do not interfere with such a determination. Ferric iron up to 2 mg per 25 ml is completely masked with ascorbic acid.Part II: Khalifa, H., and S. W. Bishara: Z. analyt. Chem. 178, 345 (1960).     

Back titration with mercuric nitrate in alkaline medium potentiometric estimation of thorium

Summary Mercuric nitrate has proved to be a suitable back titrant for EDTA amounts in excess of those reacting quantitatively with thorium amounts ranging from 46 g up to 25 mg. End points are detected potentiometrically with reasonable jumps amounting to an average of 70 mV per 0.1 ml titrant. Thorium can be determined with fair accuracy, in the presence of double its amount of uranium.