Antitumor evaluation and molecular docking study of substituted 2-benzylidenebutane-1,3-dione, 2-hydrazonobutane-1,3-dione and trifluoromethyl-1H-pyrazole analogues.

A series of 2-(arylidene)-1-(4-chlorophenyl)-4,4,4-trifluorobutane-1,3-diones (2-4), 4-(arylidene)-3-(4-chlorophenyl)-5-(trifluoromethyl)-4H-pyrazoles (5-7), 1-(4-chlorophenyl)-4,4,4-trifluoro-2-(2-(aryl)hydrazono)butane-1,3-diones (8, 9), 3-(4-chlorophenyl)-4-(2-(aryl)hydrazono)-5-(trifluoromethyl)-4H-pyrazoles (10, 11), 2-((3-(4-chlorophenyl)-1-phenyl-5-(trifluoromethyl)-1H-pyrazol-4-yl)methylene)malononitrile (13), 2-((5-(4-chlorophenyl)-1-phenyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)methylene)cycloalkan-1-ones (14, 15) and 1-(aryl)-3-(5-(4-chlorophenyl)-1-phenyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)prop-2-en-1-ones (16, 17) were designed, synthesized and evaluated for their in vitro antitumor activity. 1-(4-Chlorophenyl)-4,4,4-trifluoro-2-(2-(4-methoxyphenyl)hydrazono)butane-1,3-dione (8) showed potential and broad spectrum antitumor activity compared to the known drug 5-FU with GI50, (6.61 and 22.

Carbonic anhydrase inhibitory activity of sulfonamides and carboxylic acids incorporating cyclic imide scaffolds.

A series of sulfonamides incorporating cyclic imide moieties were investigated as inhibitors of several human α-carbonic anhydrase (hCA, EC 4.2.1.

Midurethral slings versus the standard pubovaginal slings for women with neurogenic stress urinary incontinence.

Introduction And Hypothesis: Preliminary reports show promising data on tension-free vaginal tape (TVT) in women with lower motor neuron lesion (LMNL) presenting with stress urinary incontinence (SUI). We compared efficacy and safety of TVT to pubovaginal sling (PVS) in treating SUI in women with LMNL.

Methods: This was a pilot, nonrandomized clinical trial evaluating women with SUI associated with pathology at or below S2 spinal segment.

The catalytic reactions in the Cu-Li-Mg-H high capacity hydrogen storage system.

A family of hydrides, including the high capacity MgH2 and LiH, is reported. The disadvantages these hydrides normally display (high absorption/desorption temperatures and poor kinetics) are mitigated by Cu-hydride catalysis. This paper reports on the synthesis of novel CuLi0.

Hypoxia promotes dissemination and colonization in new bone marrow niches in Waldenström macroglobulinemia.

Unlabelled: Waldenström macroglobulinemia, a rare and indolent type of non-Hodgkin lymphoma, is characterized by widespread lymphoplasmacytic B cells in the bone marrow. Previous studies have shown that hypoxic conditions play a key role in the dissemination of other hematologic malignancies. In this study, the effect of hypoxia was tested on the progression and spread of Waldenström macroglobulinemia.

The role of hypoxia and exploitation of the hypoxic environment in hematologic malignancies.

Tumor hypoxia is a well-described phenomenon during the progression of solid tumors affecting cell signaling pathways and cell metabolism; however, its role in hematologic malignancies has not been given the same attention in the literature. Therefore, this review focuses on the comparative differences between solid and hematologic malignancies with emphasis on the role of hypoxia during tumorigenesis and progression. In addition, contribution of the bone marrow and angiogenic environment are also discussed.

Primary versus secondary ureteroscopy for pediatric ureteral stones.

Objective: To evaluate the outcome of primary versus secondary ureteroscopy for pediatric ureteral stones.

Patients And Methods: A retrospective chart review study that included 66 children aged less than 12 years, who were subdivided into two groups: Group A, which included 42 children who had undergone primary ureteroscopy without pre-stenting; and Group B, which included 24 children who had undergone ureteroscopy after ureteric stenting. Kidneys, ureters and bladder radiographs were done on the first postoperative day to assess the degree of stone clearance and stent position.

Quality of life among adults with beta-thalassemia major in western Saudi Arabia.

Objectives: To assess the quality of life in the thalassemia adult patients and clarify how effective the management is of these patients and whether a change in care is warranted.

Methods: In this cross-sectional study, adult thalassemia patients (>18 years) of both genders, attending the day care unit in King Abdulaziz University Hospital, Jeedah, Saudi Arabia were surveyed using SF-36 questionnaire. Data were collected between October 2012 and December 2012.

CXCR7-dependent angiogenic mononuclear cell trafficking regulates tumor progression in multiple myeloma.

The CXCR4/stromal cell-derived factor-1 (SDF-1) axis is essential for cell trafficking and has been shown to regulate tumor progression and metastasis in many tumors including multiple myeloma (MM). A second chemokine receptor for SDF-1, CXCR7 was discovered recently and found on activated endothelial cells. We examined the role of CXCR7 in angiogenic mononuclear cells (AMCs) trafficking in MM.

Targeting survival and cell trafficking in multiple myeloma and Waldenstrom macroglobulinemia using pan-class I PI3K inhibitor, buparlisib.

The phosphatidylinositol-3 kinase (PI3K) pathway is activated in multiple myeloma (MM) and Waldenstrom Macroglobulenima (WM), and plays a crucial role in tumor progression and drug resistance. In this study, we characterized the role of pan-class I PI3K inhibition on cell trafficking and survival of MM and WM cells. We tested the effect of pan-class I PI3K inhibition by siRNA silencing or pharmacologic inhibition with buparlisib on MM cell survival, apoptosis and cell cycle in vitro and tumor growth and mobilization of MM cells in vivo.

Uropathogenic Escherichia coli isolates with different virulence genes content exhibit similar pathologic influence on Vero cells.

Uropathogenic Escherichia coli are the major causative agent of urinary tract infection--they may simultaneously express a number of virulence factors to cause disease. The aim of this study was to investigate the relation between virulence factors content of fifteen UPEC isolates and their pathogenic potential. The isolates belonged to the five serotypes O78:K80, O114:K90, O142:K86, O164 and O157.

Delivery systems for brachytherapy.

Brachytherapy is described as the short distance treatment of cancer with a radioactive isotope placed on, in, or near the lesions or tumor to be treated. The main advantage of brachytherapy compared with external beam radiation (EBR) is the improved localized delivery of dose to the target volume of interest, thus normal tissue irradiation is reduced. The precise and targeted nature of brachytherapy provides a number of key benefits for the effective treatment of cancer such as efficacy, minimized risk of side effects, short treatment times, and cost-effectiveness.

Lithium attenuates lipopolysaccharide-induced hypothermia in rats.

Background: Changes in body temperature are common features among patients with sepsis and septic shock. Similarly, systemic administration of bacterial endotoxin (lipopolysaccharide, LPS) to rats leads to an initial hypothermia followed by elevation in body temperature. These changes in body temperature are accompanied by increased levels of prostaglandin E2 (PGE2) in the hypothalamus.

The myeloid-binding peptide adenoviral vector enables multi-organ vascular endothelial gene targeting.

Vascular endothelial cells (ECs) are ideal gene therapy targets as they provide widespread tissue access and are the first contact surfaces following intravenous vector administration. Human recombinant adenovirus serotype 5 (Ad5) is the most frequently used gene transfer system because of its appreciable transgene payload capacity and lack of somatic mutation risk. However, standard Ad5 vectors predominantly transduce liver but not the vasculature following intravenous administration.

Molecularly targeted therapies in multiple myeloma.

Multiple myeloma (MM) is a hematological malignancy that remains incurable because most patients will eventually relapse or become refractory to the treatments. Although the treatments have improved, the major problem in MM is the resistance to therapy. Novel agents are currently in development for the treatment of relapsed/refractory MM, including immunomodulatory drugs, proteasome inhibitors, monoclonal antibodies, cell signaling targeted therapies, and strategies targeting the tumor microenvironment.

Effects of lithium on inflammation.

Lithium is an effective medication for the treatment of bipolar affective disorder. Accumulating evidence suggests that inflammation plays a role in the pathogenesis of bipolar disorder and that lithium has anti-inflammatory effects that may contribute to its therapeutic efficacy. This article summarizes the studies which examined the effects of lithium on pro- and anti-inflammatory mediators.

4-[(1,3-Dioxoisoindolin-2-yl)meth-yl]benzene-sulfonamide.

The title compound, C15H12N2O4S, is V-shaped with the isoindoline ring system (r.m.s.

3-Amino-5,5-di-phenyl-imidazolidine-2,4-dione.

The title compound, C15H13N3O2, crystallizes with two independent mol-ecules in the asymmetric unit, which differ considerably in the dihedral angles made between the phenyl groups and the five-membered rings [47.19 (8) and 61.16 (9)° in one mol-ecule and 55.

N-(12-Amino-9,10-di-hydro-9,10-ethano-anthracen-11-yl)-4-methyl-benzene-sulfonamide.

The title compound, C23H22N2O2S, crystallizes with the 4-methyl-benzene-sulfonamide entity oriented towards the center of the bridgehead C atoms with a C-N-S-C torsion angle of -61.3 (2)°. The mol-ecule features an intra-molecular N-H⋯N hydrogen bond.

2-Meth-oxy-4,6-di-phenyl-nicotino-nitrile.

In the title compound, C19H14N2O, the phenyl rings form dihedral angles of 10.90 (10) and 42.14 (6)° with pyridine ring and an angle of 35.

3-[2-(4-Fluoro-phen-yl)-2-oxoeth-yl]-5,5-di-phenyl-imidazolidine-2,4-dione.

The title compound, C23H17FN2O3, crystallizes with two independent mol-ecules in the asymmetric unit. The mol-ecules are connected by pairs of N-H⋯O hydrogen bonds and have slightly different conformations, as indicated by the dihedral angles between the central imidazolidine-2,4-dione ring and its three substituents. In one mol-ecule, these are 60.

1-Acetyl-5-meth-oxy-4-(phenyl-sulfan-yl)imidazolidin-2-one.

The title compound, C12H14N2O3S, crystallizes with two independent mol-ecules (A and B) in the asymmetric unit. The five-membered imidazolidin-2-one rings in both mol-ecules are twisted about the C-C bond. In the crystal, the A and B mol-ecules are associated via pairs of N-H⋯O hydrogen bonds, forming A-B dimers.

Design, synthesis and biological evaluation of some novel substituted quinazolines as antitumor agents.

A novel series of 6-chloro-2-p-tolylquinazolinone and substituted-(4-methylbenzamido)benzamide (1-20) were designed, synthesized and evaluated for their in-vitro antitumor activity. Compounds 3, 14 and 16 possessed remarkable broad-spectrum antitumor activity. Compound 16 was found to be a particularly active growth inhibitor of the renal cancer (GI50 = 4.

The role of P-glycoprotein in drug resistance in multiple myeloma.

Multiple myeloma (MM) is a malignant neoplastic cancer of the plasma cells that involves the bone marrow. The majority of patients with MM initially respond to chemotherapy, but they eventually become resistant to later drug therapy. One of the reasons for drug resistance in patients with MM is efflux transporters.