Search results for "TOPS"

Progressive calcifications of lung and liver in neonatal herpes simplex virus infection

1991

We report a female neonate who developed severe septicemia presenting with pneumonia and hepatitis due to an infection with herpes simplex virus type II. In spite of antiviral as well as intensive care therapy, three weeks after admission, extensive hepatic calcification was demonstrable on abdominal radiograph, a sign of severe cellular necrosis. In contrast the pulmonary infiltration recovered completely. The clinical follow up was completed by ultrasound and radiography. The infant died at the age of two months secondary to severe postnecrotic hepatic failure. At autopsy, histological evaluation confirmed the former diagnostic and technical findings; in addition, pulmonary calcifications…

Latvijas ūdeņu vides pētījumi un aizsardzība: Referātu tēžu krājums

2016

Early calcification patterns of the iliac arteries and their relation to the arterial structure

1972

Gross calcifications of the common iliac and internal iliac arteries represent a common finding in newborn children and infants. In both arteries, the calcific deposits regularly appear in certain areas of the arterial luminal surface only, whereas the other parts of the arterial wall remain free of gross lesions even in cases with a pronounced calcification. In the common iliac artery, the lateral wall of the vessel and the adjacent sectors of the anterior and posterior wall represent the predilection site of calcific deposits. In the internal iliac artery, the gross calcifications have been regularly demonstrated in the dorso-medial wall. The predominant localisation of the calcification …

Influence of vegetation recovery on soil hydrology and erodibility following fire: an 11-year investigation

2005

The present study investigates long-term changes in soil hydrological properties and erodibility during the regrowth of different types and densities of vegetation following a severe wildfire in the Serra Grossa Range, eastern Spain. Twelve plots of similar slope and soil characteristics, naturally recolonized by four different plant species (trees, herbs, shrubs and dwarf shrubs) were examined using rainfall simulations during an 11-year period. The mean erosion rate was 80 g m−2 h−1, 6 months after the fire under wet-winter conditions, declining to 30 g m−2 h−1 in the following summer and reaching <10 g m−2 h−1 after 2 years. Considerable variation under the different vegetation types …

Pedogenesis and Variability in Soil Properties in a Floodplain of a Semiarid Environment in Southwestern Sicily (Italy).

2010

We performed a pedological study of the variability in soils in a floodplain area of a semiarid region in southwestern Sicily. The objectives of our research were to (i) investigate the role of parent material, erosion, and distribution processes on soil pedogenesis and horizon differentiation; (ii) evaluate the statistical distribution of soil properties; and (iii) interpret these distributions in terms of pedogenic and other processes. Our results showed that not all soil properties examined followed a normal distribution and that even when logtransformed, the degree of normality of the soil salinity data did not improve. Furthermore, principal component analysis was performed to investig…

1,2,4-Oxadiazole topsentin analogs as staphylococcal biofilm inhibitors targeting the bacterial transpeptidase sortase A

2020

The inhibition or prevention of biofilm formation represents an emerging strategy in the war against antibiotic resistance, interfering with key players in bacterial virulence. This approach includes the inhibition of the catalytic activity of transpeptidase sortase A (Srt A), a membrane enzyme responsible for covalently attaching a wide variety of adhesive matrix molecules to the peptidoglycan cell wall in Gram-positive strains. A new series of seventeen 1,2,4-oxadiazole derivatives was efficiently synthesized and screened as potential new anti-virulence agents. The ability of inhibiting biofilm formation was evaluated against both Gram-positive and Gram-negative pathogens. Remarkably, all…

3-[4-(1H-indol-3-yl)-1,3-thiazol-2-yl]-1H-pyrrolo[2,3-b]pyridines, nortopsentin Analogues with antiproliferative activity

2015

A new series of nortopsentin analogues, in which the imidazole ring of the natural product was replaced by thiazole and the indole unit bound to position 2 of the thiazole ring was substituted by a 7-azaindole moiety, was efficiently synthesized. Two of the new nortopsentin analogues showed good antiproliferative effect against the totality of the NCI full panel of human tumor cell lines (~60) having GI50 values ranging from low micromolar to nanomolar level. The mechanism of the antiproliferative effect of these derivatives, investigated on human hepatoma HepG2 cells, was pro-apoptotic, being associated with externalization of plasma membrane phosphatidylserine and mitochondrial dysfunctio…

Synthesis and Antitumor Activity of 3-(2-Phenyl-1,3-thiazol-4-yl)-1H-indoles and 3-(2-Phenyl-1,3-thiazol-4-yl)-1H-7-azaindoles

2011

Given the potent antimicrobial, antiviral, and antitumor activities of many natural products, there is an increasing interest in the synthesis of new molecules based on natural compound scaffolds. Based on a 2,4-bis(3'-indolyl)imidazole skeleton, two new series of phenylthiazolylindoles and phenylthiazolyl-7-azaindoles were obtained by Hantzsch reaction between substituted phenylthioamides and the α-bromoacetyl derivatives. Some azaindole derivatives, tested at the National Cancer Institute against a panel of ∼60 tumor cell lines derived from nine human cancer cell types, showed inhibitory effects against all cell lines investigated at micromolar to nanomolar concentrations. Two of them exh…

A Facile Synthesis of Deaza-Analogues of the Bisindole Marine Alkaloid Topsentin

2013

A series of substituted ethyl 1-[(tert-butoxycarbonyl)amino]-2-methyl-5- (1-methyl-1H-indol-3-yl)-4-[(1-methyl-1H-indol-3-yl)carbonyl]-1H-pyrrole-3-carboxylates were prepared in excellent yields (82-98%) by one-pot reactions between β-dicarbonyl compounds 12a-e and 1,2-diaza-1,3-diene (DD) 13. Derivatives 10a,c-e, deazaanalogues of the bis-indole alkaloid topsentin, screened by the National Cancer Institute (Bethesda, MD, USA) in the in vitro one dose primary anticancer assay against a panel of about 60 human tumor cell lines, showed no significant activity, with the exception of compound 9e, which showed moderate activity against the HOP-92 cell line of the non small cell lung cancer sub-p…

A New Oxadiazole-Based Topsentin Derivative Modulates Cyclin-Dependent Kinase 1 Expression and Exerts Cytotoxic Effects on Pancreatic Cancer Cells

2021

Pancreatic ductal adenocarcinoma (PDAC) is a highly lethal form of cancer characterized by drug resistance, urging new therapeutic strategies. In recent years, protein kinases have emerged as promising pharmacological targets for the treatment of several solid and hematological tumors. Interestingly, cyclin-dependent kinase 1 (CDK1) is overexpressed in PDAC tissues and has been correlated to the aggressive nature of these tumors because of its key role in cell cycle progression and resistance to the induction of apoptosis. For these reasons, CDK1 is one of the main causes of chemoresistance, representing a promising pharmacological target. In this study, we report the synthesis of new 1,2,4…