Synthesis of Benzophenones and in vitro Evaluation of Their Anticancer Potential in Breast and Prostate Cancer Cells

Breast and prostate cancers are frequently treated with chemotherapy. Several novel chemicals are being reported for this purpose, particularly synthetic and natural benzophenones. This work reports the synthesis of substituted 2-hydroxybenzophenones through 1,4-conjugate addition/intramolecular cycloaddition/dehydration of nitromethane on key intermediate chromones. Structures were extensively studied by means of 2D NMR spectroscopy and single-crystal XRD. Their cytotoxicity was evaluated in vitro in two breast cancer cell lines (MDA-MB-231 and T47-D) and one prostate cancer cell line (PC3). The most potent compound exhibited good cytotoxic effects against the three cancer cell lines (IC₅₀ values ranging from 12.09 to 26.49 μm ) and induced cell-cycle retardation only on prostate cancer cells, which suggested that it might exert cell-type-specific effects.     

Minors held by majors: the H13 minor histocompatibility locus defined as a peptide/MHC class I complex

The products of minor histocompatibility (H) loci are serious barriers to tissue transplantation even among major histocompatibility complex (MHC) identical individuals, frequently causing chronic graft rejection and graft versus host disease. Over 50 minor H loci map to mouse autosomal chromosomes but none are known at the molecular level. By expression cloning, we identified the H13 locus, a classical minor H locus first detected 30 years ago by the trait of graft rejection. The H13a allele is located on chromosome 2 and encodes a novel protein that yields the rare naturally processed nonapeptide SSVVGVWYL (SVL9) for presentation by the Db MHC class I molecule. The SVL9 peptide binds Db MHC despite the absence of the consensus binding motif, and a conservative methyl group substitution (Valine 4 <--> Isoleucine) explains why reciprocal T cell responses are elicited in H13a and H13b congenic strains.     

Multidrug resistance-reversing agents increase vinblastine distribution in normal tissues expressing the P-glycoprotein but do not enhance drug penetration in brain and testis

The aim of this study was to assess whether P-glycoprotein (Pgp) inhibitors altered the blood-brain barrier and enhanced vinblastine (VBL) distribution in brain, testis and other Pgp-expressing tissues. Trifluoperazine, cyclosporin A, amiodarone, quinidine, the nifedipine analog Bay K8644 and verapamil were selected among Pgp inhibitors and were administered intraperitoneally 1 hr before an intravenous dose of 10 mg/kg VBL. Trifluoperazine and cyclosporin A were also administered intraperitoneally for 7 days before VBL. VBL and its metabolite O4-deacetylvinblastine were measured in tissues by high-performance liquid chromatography assay. None of the reversing agents (RA) appreciably raised VBL concentrations in brain and testis, whereas all except quinidine significantly enhanced VBL distribution in liver and kidney; the most effective were trifluoroperazine and cyclosporin A. In mice treated with RA and VBL combined, O4-deacetylvinblastine levels in liver and kidney reached either the same or higher levels than in mice treated with VBL alone, indicating that the increase in VBL levels is not due to inhibition of its metabolism. The main conclusions are that (1) inhibitors of Pgp, even at high doses, do not increase the permeability of the blood-brain barrier in mice, suggesting caution in the clinical use of RA combined with antitumor agents for brain tumors; and (2) several RA achieve high enough concentrations to enhance the distribution of VBL in other normal tissues expressing Pgp, thus potentially increasing VBL toxicity.     

On mapping processes to processors in distributed systems

This paper is concerned with the implementation of parallel programs on networks of processors. In particular, we study the use of the network augmenting approach as an implementation tool. According to this approach, the capabilities of a given network of processors can be increased by adding some auxiliary links among the processors. We prove that the minimum set of edges needed to augment a line-like network so that it can accommodate a parallel program is determined by an optimal path cover of the graph representation of the program. Anoptimal path cover of a simple graphG is a set of vertex-disjoint paths that cover all the vertices ofG and has the maximum possible number of edges. We present a linear time optimal path covering algorithm for a class of sparse graphs. This algorithm is of special interest since the optimal path covering problem is NP-complete for general graphs. Our results suggest that a cover and augment scheme can be used for optimal implementation of parallel programs in line-like networks.A preliminary version of this paper was presented at the 6th IEEE Conference on Computer Communications (INFOCOM '87).This reseach is supported in part by National Semiconductor (Israel), Ltd.     

Switching to Directional Antennas with Constant Increase in Radius and Hop Distance

For any angle α<2π, we show that any connected communication graph that is induced by a set P of n transceivers using omni-directional antennas of radius 1, can be replaced by a strongly connected communication graph, in which each transceiver in P is equipped with a directional antenna of angle α and radius r _dir, for some constant r _dir=r _dir(α). Moreover, the new communication graph is a c-spanner of the original graph, for some constant c=c(α), with respect to number of hops.     

Activation of Pozzolanic Reaction of Hydrated Portland Cement Fly Ash Pastes in Sulfate Solution

The activation of the pozzolanic reaction of fly ash in portland cement paste immersed in sulfate solution has been studied. Mixtures of two Spanish fly ashes (ASTM class F) with 0%, 15%, and 35% replacement of portland cement by fly ash were immersed in Na₂SO₄ solution, of 2880 ppm SO₄²⁻ concentration, for a period of 90 days. The resistance of the different mixtures to the sulfate attack was evaluated using the Koch-Steinegger test. The results showed that all of the mixtures were sulfate resistant, despite the high Al₂O₃ content of the fly ash. The diffusion of SO₄²⁻ and Na⁺ ions through the pore solution activated the pozzolanic reactivity of the fly ashes, causing microstructural changes, which were characterized by X-ray diffraction (XRD), mercury intrusion porosimetry (MIP), and scanning electron microscopy (SEM). As a result, the flexural strength of the mixtures increased, principally for the fly ash of a lower particle size and 35% of addition.     

Some practical aspects connected with the presence of calcium in soybean oils

Presence of calcium in crude and degummed soybean oils prevents complete elimination of phosphatides by hydration and enhances the formation of heavy precipitates. They block industrial centrifuges at the later stages of the refining processes. Industrially extracted degummed soybean oils contain appreciable amounts of calcium (ca. 100 ppm) and its source was traced to the processed soybeans. Various pre-extraction treatments of the soybeans in industry augment the calcium content in the oils, since crude Soxhlet-extracted soybean oils contained only 15 ppm calcium. Additions at the alkali-refining stages of EDTA or of polyphosphate, to stabilize aqueous suspensions which also contain calcium salts, are suggested as a partial remedy to the frequent blocking of the centrifuges.     

An Experimental Approach for the Characterisation of Rigid Porous Media and Unsaturated Conductivity Relations

A laboratory procedure for the characterisation of rigid, porous media is developed and tested. The overall objective of the characterisation is to provide a basis for the choice of a relevant unsaturated conductivity relation. With the proposed procedure, the porous materials are characterised through hydraulic conductivity measurements, saturation-pressure measurements, porosity measurements and air entry pressure measurements. The measurements were conducted using water and a selected non-aqueous phase liquid (n-decane), and two types of homogeneous, rigid porous media of different origin (fritted glass samples with guaranteed homogeneity by the manufacturer, and chalk). The laboratory method successfully characterised the fritted glass samples as homogeneous on basis of calculated tortuosity values, measured bubble pressures and measured pore-size density curves. The contact angle between the liquid and the solid had negligible impact when comparing the drainage of water with the drainage of n-decane, and also when comparingn -decane drainage in dry porous media withn -decane drainage in media where a film of water separated then -decane from the pore wall. Also, the differences in saturated conductivities between n-decane and water in both samples of chalk and fritted glass were well predicted on basis of differences in density and viscosity of the liquids. The laboratory procedure was furthermore used for characterisation of the pore space available for non-aqueous liquid flow in partially water-saturated porous media. Then -decane conductivities in the fritted glass samples partially saturated with water were considerably lower than the n-decane conductivities in the dry fritted glass samples.