The infrared (4000–200 cm−1) spectrum for 4-amino-5-pyrimidinecarbonitrile (APC, C5H4N4) was acquired in the solid phase. In addition, the 1H and 13C NMR spectra of APC were obtained in DMSO-d6 along with its mass spectrum. Initially, six isomers were hypothesized and then investigated by means...

A series of eight N4-phenylsubstituted-6-(2,4-dichlorophenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines 8–15 were synthesized as vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors with varied substitutions in the phenyl ring of the 4-anilino moiety. In addition, five N4-phe...

This work describes a solid-phase synthetic method for building a compound library of N-alkyl-4-alkylamino-1-aryl-1H-pyrazolo[3,4-d]pyrimidine-6-carboxamide derivatives, that are based on the biologically active 1-aryl-1H-pyrazolo[3,4-d]pyrimidine scaffold. In the first step of this synthetic se...

Six novel N4-substitutedphenyl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines were synthesized as multiple receptor tyrosine kinase (RTK) inhibitors and antitumor agents. An improvement in the inhibitory potency against epidermal growth factor receptor (EGFR), vascular endoth...

Checkpoint kinase 1 (CHK1) inhibitors can potentiate the effectiveness of deoxyribonucleic acid (DNA) damaging agents in the treatment of cancer. A novel series of 2,6-disubstituted-9H-purine (3a-p, 5a and 5b), 2,4-disubstituted-thieno[3,2-d]pyrimidine (8a-c) and 2,4-disbustituted-7H-pyrrolo[2,3...

The two natural 1,3,5-undecatrienes have been synthesized starting from pyridazine-1-oxide. The method allows us to obtain a mixture, in which the 1, 3E, 5Z isomer predominates.

Two new and short syntheses of (3E,5Z)-1,3,5-undecatriene 1 are presented. Both approaches are based on the coupling between a C7 and a C4 synthon and afford 1 in 92–96% stereoisomeric purity.

A new synthesis of (3E, 5Z)-1,3,5-undecatriene (2) is presented, based on a Mannich addition to 1,4 decadiyne, followed by Lindlar hydrogenation and Hofmann elimination. This “one pot” coupling of C7+C3+C1 synthons affords 2 stereochemically pure.

In dimethylformamide containing tetramethylammonium perchlorate, reduction of 1,10-diiododecane yields two irreversible voltammetric waves at mercury, whereas reduction of 1,10-dibromodecane gives only one irreversible wave. Quantitative comparison of this behavior with that known for 1-iodo- an...

A short-term (24 h) method of gill filament culture system was developed to predict the effects of environmental contamination and stress in fish. Gill culture system containing two or three rainbow trout gill filaments in sterile glutamine supplemented Leibovitz 15 (L-15) media was submitted fo...

BackgroundSerine racemase (SR) catalyzes the production of d-serine, a co-agonist of the N-methyl-d-aspartate receptor (NMDAR). A previous report shows the contribution of SR in the NMDAR-mediated neuronal cell death process.

O-(5-Acetamido-3,5-dideoxy-d-glycero-α-d-galacto-2-nonulopyranosylonic acid)-(2→6)-O-(2-acetamido-2-deoxy-α-d-galactopyranosyl)-(1→3)-l-serine, a structural unit occurring in various submaxillary mucins, was synthesized for the first time by using O-[methyl (5-acetamido-4,7,8,9-tetra-O-acety...

N-(Benzyloxycarbonyl)-O-[methyl (5-acetamido-4,7,8,9-tetra-O-acetyl-3,5- dideoxy-d-glycero-α-d-galacto-2-nonulopyranosyl)onate]-(2→3)-O-(2,4,6-tri-O- acetyl-β-d-galactopyranosyl)-(1→3)-O-[methyl (5-acetamido-4,7,8,9-tetra-O- acetyl-3,5-dideoxy-d-glycero-α-d-galacto-2-nonulopyranosyl)onate-(...

The enthalpies of dilution of five dipeptides, namely, N-aeetyl-N '-methyl amides of l-serine, l-threonine and l-hydroxyproline, and JV-acetyl amides of l-threonine and l-hy-droxyproline dissolved in N, N-dirnethylformamide were measured calorimetrically at 298.15 K. From these, the enthalp...

N-Acetyl-l-serine (NAS) is a component of dietary proteins and a minor constituent of foods as a free amino acid. The current paper reports the outcome of toxicology studies conducted to assess the safety of NAS. No evidence of mutagenicity was observed in the reverse bacterial mutation assay. G...

The spectroscopic parameters of the paramagnetic species produced in gamma-irradiated l-citrulline, α-methyl-dl-serine, 3-fluoro-dl-valine and N-acetyl-l-cysteine were investigated at room temperature at a dose of 20 kGy by using EPR technique. The paramagnetic species were attributed to NH2CON...

A simple model is proposed for the calculation of oil and water mutual solubilities as a function of temperature using the hydrocarbon specific gravity and Watson-K factor as correlating parameters. The model parameters were determined using a single consistent set of high quality solubility dat...

The metabolism of 7,12-dimethylbenz[a]anthracene (DMBA) and its non-carcinogenic 2-fluoro analogue (2F-DMBA) by Syrian hamster embyro (SHE) cells has been studied using high pressure liquid chromatography (HPLC) and fluorescence spectroscopy. Metabolites produced by SHE cells were compared chrom...

Effects of the green tea catechins (GTCs) on the late promotion or progression stage of mammary gland carcinogenesis were examined in female Sprague-Dawley (SD) rats pretreated with 7,12-dimethylbenz(a)anthracene (DMBA). A total of 84 7-week-old rats received a 50 mg/kg body weight intra-gastric...

The effects of 7-alkyl substitution on the reversible intercalation of the proximate carcinogen trans-3,4-dihydroxy-3,4-dihydrobenz[a]anthracene (BAD) to calf thymus DNA have been examined using time-resolved fluorescence spectroscopy. The results indicate that in 10−3 M sodium cacodylate the bi...