The alpha 6 beta 1 integrin is expressed on the macrophage surface in an inactive state and requires cellular activation with PMA or cytokines to function as a laminin receptor (Shaw, L. M., J. M. Messier, and A. M. Mercurio. 1990. J. Cell Biol. 110:2167-2174). In the present study, the role of the alpha 6 subunit cytoplasmic domain in alpha 6 beta 1 integrin activation was examined. The use of...

Pyrazolopyranopyrimidines 6a-c and 8a-c were prepared from the reaction of compounds 4a-c or 7a-c with methylamine or ammonium hydroxide solutions. Treatment of compounds 6a-c or 8a-c with 2-chloroethyl methyl ether afforded their corresponding acyclonucleosides 9a-c or 10a-c, respectively, as a new class of acyclonucleosides. All prepared compounds were tested as anti-inflammatory agents and s...

Fifteen novel β-lactams bearing the N-ethyl tert-butyl carbamate group 5a-o and fifteen N-(2-aminoethyl) β-lactams 6a-o were synthesized by the ketene-imine [2+2] cycloaddition reaction (Staudinger ). The cycloaddition reaction was found to be totally diastereoselective leading exclusively to the formation of the cis-β-lactam derivatives. These newly synthesized β-lactams were evaluated for the...

The ability of the hydrosoluble ruthenium(II) complexes [RuCl2(h-arene)(PTA)] 3a–d, [RuCl2(h-arene)(PTA-Bn)] 4a–d, [RuCl2(h-arene)(DAPTA)] 5a–d, [RuCl2(h-arene)(TPPMS)] 6a–d (arene = C6H6, p-cymene, 1,3,5-C6H3Me3, C6Me6) to promote the atom-economic formation of b-oxo esters, by addition of carboxylic acids to terminal propargylic alcohols in water has been explored. Scope, limitations and cata...

PURPOSE The aim of this study was to investigate the functions of dsRNA-activated protein kinase (PKR) in choroidal neovascularization (CNV) and related signaling pathways in the production of vascular endothelial growth factor (VEGF). METHODS A chemical hypoxia model of in vitro RF/6A cells, a rhesus choroid-retinal endothelial cell line, was established by adding cobalt chloride (CoCl2) to ...

A highly efficient method for the construction of 3a,6a-dihydrofuro[2,3-b]furan derivatives has been developed via a novel bicyclization, which is very valuable for the synthesis of fused furofuran compounds since it is time-saving and catalyst-free. Based on the bicyclization, a coupled domino strategy has been developed to directly construct 3a,6a-dihydrofuro[2,3-b]furan derivatives from meth...

The glyceride ester derivatives 6a and 6b were prepared by reacting 1,2,3-trihydroxy propane 1,3-dipalmitate/stearate with (S)-naproxen as potential prodrugs. The synthesis was achieved successfully with the aid of N,N’-dicyclohexylcarbodiimide. These prodrugs were evaluated for anti inflammatory, analgesic and gastroprotective activity. It was found that prodrugs 6a and 6b showed less irritati...

A series of substituted 4-oxopyrido[2,3-a]phenothiazine-3-carboxylic acids (6a-d) were prepared via cyclization of the corresponding ethyl 7-(arylthioxy)-8-nitro(or azido)-4-oxoquinoline-3-carboxylates (3a-d/4a-d), followed by hydrolysis of the resultant esters (5a-d). Among these tetracyclics, compound 6a with unsubstituted terminal benzo-ring D was the most active against representative Gram-...

A series of 3-[alpha-(acylamino)acyl]-1-aryl-3-methyltriazenes 6a-l, potential cytotoxic triazene prodrugs, were synthesised by coupling 1-aryl-3-methyltriazenes to N-acylamino acids. Their hydrolysis was studied in isotonic pH 7.4 phosphate buffer and in human plasma, while hydrolysis of the derivative 6a was studied in more depth across a range of pH values. Prodrugs 6a-l hydrolyse by cleavag...