A new versatile reagent, 3-bromopropylamine, for the quantitative analysis of cysteine residues in proteins and peptides is reported. When added to amino acid standards, the 3-bromopropylamine derivative of cysteine, S-3-aminopropylcysteine, elutes in a unique position on four different amino ac...

Publisher SummaryThis chapter describes the alkylation of cysteine residues with 3-bromopropylamine, and identification by protein sequencing and quantitation by amino acid analysis. It discusses the alkylation conditions for proteins in situ on sequencer membranes that are convenient, efficient...

In contrast to the corresponding hydroxyiodination reactions, the reaction of acetoxycyclohex-2-ene 1 with N-PSP in the presence of water shows little regiocontrol, but is highly diastereoselective. However, the same reaction of the (R)-phenylglycinate derivative of (±)-cyclohexen-3-ol is highl...

The hydrogen absorption and desorption properties of a MgH2 – 1 mol.% Nb(V) ethoxide mixture are reported. The material was prepared by hand mixing the additive with previously ball-milled MgH2. Nb ethoxide reacts with MgH2 during heating, releasing C2H6 and H2, and producing MgO and Nb or Nb h...

The effect of titanium isopropoxide (TTIP) on the kinetics of absorption and desorption of magnesium hydride was compared to the benchmark additive niobium oxide (Nb2O5). A systematic survey was performed for ball-milled MgH2 mixed with up to 2 mol% TTIP or Nb2O5 additive for different ball-mill...

The coordination behavior of 2-chloro-4-fluorobenzoate and 2,4-dichlorobenzoate ligands towards copper(II) ion were investigated in the presence of different nitrogen ligands. Four new copper(II) complexes, [trans-Cu(2-Cl-4-FC7H3O2)2(β-pic)2] 1, [trans-Cu(en)2(H2O)2](2-Cl-4-FC7H3O2)2, 2, [trans...

Three new copper(II) complexes trans-[Cu(β-pic)2(H2O)2(5-chloro-2-nitrobenzoate)2] 1, trans-[Cu(γ-pic)2(5-chloro-2-nitrobenzoate)2], 2 and [trans-Cu(en)2(H2O)2](5-chloro-2-nitrobenzoate)2·2H2O, 3 (where β-pic = β-picoline, γ-pic = γ-picoline and en = ethylenediamine) were prepared by the ...

Solvent effects on 2-hydroxy-4-methyl-3-nitropyridine molecule in different solvents (benzene, toluene, chloroform, acetone and water) were studied theoretically at the DFT/B3LYP level in combination with the conductor polarizable continuum model (CPCM) for the first time. Based on these results...

A class of substituted 1-thiazol-2-yl-N-3-methyl-1H-pyrozole-5-carboxylic acid derivatives was found to have potent anti-proliferative activity against a broad range of tumor cell lines. A compound from this class (14) was profiled across a broad panel of hematologic and solid tumor cancer cell ...

An N-Substituted 1H-indole derivative having an empirical formula C16H13NO3S was synthesized by the condensation of 2-Methyl-1H-Indole-3-carbaldehyde and benzene sulfonyl chloride in presence of a phase transfer catalyst of type quaternary ammonium salt in basic conditions. Then the compound was...

Quantum chemical calculations on energy and molecular structure of 2-amino-3-methyl-5-nitropyridine (2A3M5NP) have been attempted by implementing DFT/B3LYP method using 6-311G (d,p), 6-311G++ (d,p) and cc-pVTZ basis sets. The optimized geometry and the vibrational analysis for energetically most...

The developed procedure is based on the interaction of isoniazid with 2-methyi-3-nitropyridine-6-carboxaldehyde at room temperature. The colour intensity of the reaction product was quantified spectrophotometrically at 385 nm with a lower limit of detection of 0.5 μg/ml. The colour is stable fo...

A sensitive, selective colorimetric assay was developed for the quantitative analysis of dihydralazine sulfate. The method is based on the interaction of buffered (pH 4) dihydralazine sulfate with a methanolic solution of 2‐methyl‐3‐nitropyridine‐6‐carboxaldehyde upon heating to give an ora...

The hexaruthenium cluster complexes [Ru6(μ3-H)(μ5-κ2-L)(μ- CO)(CO)15], HL = 2-mercaptopyridine (1) and 2-mercapto-6-methylpyridine (2), have been prepared by heating [Ru3(CO)12] with 0.5 equiv. of HL in THF at reflux temperature. An X-ray diffraction study on a crystal of complex 2 has deter...

A novel series of BTK inhibitors bearing thieno[3,2-c]pyridin-4-amine framework as the core scaffold were designed, synthesized and well characterized. In this paper, twenty one compounds displayed variant inhibitory activities against BTK in vitro, and compound 14g showed the most potent inhibi...

A series of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent BTK inhibitors were designed, synthesized and evaluated. These thieno[3,2-c]pyridin-4-amine derivatives displayed variant inhibitory activities against BTK in vitro. Among these, 7-pyrazol-4-yl substituted...

Transforming growth factor (TGF-β), a key mediator of tumor growth and metastasis, has been recognized as an important cancer drug target. A series of benzo[c][1,2,5]thiadiazol-5-yl imidazoles (14a–g) and thieno[3,2-c]-pyridin-2-yl imidazoles (20a–g) were designed, synthesized, and evaluated ...

New indolyloxypropanolamines in which the substituent at the side chain nitrogen atom was the 2-(1H- indol-3yl)-1,1-dimethylethyl group have been synthesized as putative anti-hypertensive agents. In vitro assays were used to measure their affinity for the β1-, β2, α1- and α2-adrenoceptors, w...

We report the synthesis of a single enantiomer of an α-methyl-trans-cyclopropane unit present in a number of mycolic acids and its incorporation into a reported 1,2-dialkylcyclopropane meromycolate that contains one cis-1,2-dialkylcyclopropane and one α-methyl-trans-1,2-dialkylcyclopropane.

Two phosphorescent iridium(III) complexes (dfpmpy)2Ir(ppc) and (dfpmpy)2Ir(prz) [dfpmpy=2-(2′,4′-difluorophenyl)-4-methylpyridine, ppc=pipecolinate, prz=2-pyrazine carboxylate] were synthesized from the reaction of the chloro-bridged dimeric complex [(dfpmpy)2Ir(μ-Cl)]2 and the ancillary liga...