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.     

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.     

Synthesis of UHMW-PE by a Highly Active Homogeneous System: η5-(C5H5)2Ti(η1-OC(O)C6H5)2/MAO

Summary The complex ⁵-(C₅H₅)₂Ti (¹-OC(O)C₆H₅)₂ was synthesized and activated with MA0 for ethylene polymerization. The resultant polymer is UHMW-PE with a viscosimetric molecular weight of Mv = 6.8 x 10⁶ to 0.7 x 10⁶ g/mol dependent on the temperature of the reaction. The effects of the Al/Ti molar ratio and temperature of the reaction on the catalytic activity and polymer properties were studied.     

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.     

Analyzing the performance of a cluster-based architecture for immersive visualization systems

Cluster computing has become an essential issue for designing immersive visualization systems. This paradigm employs scalable clusters of commodity computers with much lower costs than would be possible with the high-end, shared memory computers that have been traditionally used for virtual reality purposes. This change in the design of virtual reality systems has caused some development environments oriented toward shared memory computing to require modifications to their internal architectures in order to support cluster computing. This is the case of VR Juggler, which is considered one of the most important virtual reality application development frameworks based on open source code.     

A new system architecture for crowd simulation

Crowd simulation requires both rendering visually plausible images and managing the behavior of autonomous agents. Therefore, these applications need an efficient design that allows them to simultaneously handle these two requirements. Although several proposals have focused on the software architectures for these systems, no proposals have focused on the computer systems supporting them.In this paper, we analyze the computer architectures used in the literature to support distributed virtual environments. Also, we propose a distributed computer architecture which is efficient enough to support simulations of thousand of autonomous agents. This proposal consists of a cluster of interconnected computers in order to improve flexibility and robustness, as well as a hierarchical software architecture that efficiently provides consistency. Performance evaluation results show that the trade-off between flexibility and consistency allows to efficiently manage thousands of autonomous agents. Therefore, this network-based system architecture can provide the required scalability for large-scale crowd simulations.