Search results for "AZO"

MTOR inhibitor-based combination therapies for pancreatic cancer

2018

Background: Although the mechanistic target of rapamycin (MTOR) kinase, included in the mTORC1 and mTORC2 signalling hubs, has been demonstrated to be active in a significant fraction of patients with pancreatic ductal adenocarcinoma (PDAC), the value of the kinase as a therapeutic target needs further clarification. Methods: We used Mtor floxed mice to analyse the function of the kinase in context of the pancreas at the genetic level. Using a dual-recombinase system, which is based on the flippase-FRT (Flp-FRT) and Cre-loxP recombination technologies, we generated a novel cellular model, allowing the genetic analysis of MTOR functions in tumour maintenance. Cross-species validation and pha…

Thiazole Analogues of the Marine Alkaloid Nortopsentin as Inhibitors of Bacterial Biofilm Formation

2020

Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections that are biofilm-mediated, new therapeutic agents capable of counteracting the formation of biofilms are urgently required. In this scenario, a new series of 18 thiazole derivatives was efficiently synthesized and evaluated for its ability to inhibit biofilm formation against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923 and S. aureus ATCC 6538 a…

Crystal structure and Hirshfeld surface analysis of (Z)-4-chloro-N′-(4-oxothiazolidin-2-ylidene)benzenesulfonohydrazide monohydrate

2018

The asymmetric unit of the title thiazole derivative containing a sulfonylhydrazinic moiety, C9H8ClN3O3S2·H2O, consists of two independent molecules and two water molecules. The central parts of the molecules are twisted as both the molecules are bent at both the S and N atoms. In the crystal, N—H...N, N—H...O, C—H...O and O—H...O hydrogen-bonding interactions connect the molecules, forming layers parallel to the ab plane. Two-dimensional fingerprint plots associated with the Hirshfeld surface show that the largest contributions to the crystal packing come from O...H/H...O (32.9%) and H...H (22.6%) interactions.

Synthesis and anticancer activity of new thiazole nortopsentin analogues

2015

Thiazolium salts as catalysts for etherification reaction

2014

Rhizoctonia solani AG5 and Its Offspring – Morphology and Sensitivity to Fungicides

2022

The objective of these studies was to identify differences and similarities within the progeny of Rhizoctonia solani AG5, which arose from basidiospores produced by the maternal strain ID23. The following characteristics were analyzed: appearance of the mycelium (color, structure, zonation, and presence of sclerotia), growth rate (at 10°C, 20°C, and 30°C), fungicide sensitivity, and hyphal structure. The mycelial color of R. solani AG5 ranged from white/cream to light and dark brown. The structure of the mycelium may be compacted or flattened with visible zoning or fluffy with dark brown sclerotia on the colony surface. Homokaryons and heterokaryons derived from homokaryons were analyzed by…

Synthesis, antiproliferative activity, and in silico insights of new 3-benzoylamino-benzo[ b ]thiophene derivatives

2014

A new series of 3-benzoylamino-5-imidazol-5-yl-benzo[b]thiophenes and the parent amino derivatives were synthesized and screened as antitumor agents. All tested compounds showed concentration-dependent antiproliferative activity profile against HeLa cell line, exhibiting GI50 values in the low micromolar range. The most active compounds were tested in cell cycle perturbation experiments. A rapid accumulation of cells in the G2/M phase, with a concomitant reduction of cells in both the S and G0/G1 phases, was observed, suggesting that cell exposure to selected derivatives produces mitotic failure. To rationalize the biological results, the 3-benzoylamino-benzo[b]thiophenes were analyzed thro…

A competitive reactivity study on the oxidative cyclization of thiosemicarbazones into 1,3,4-thiadiazoles

2022

Abstract In order to obtain useful insights on the mechanism of formation of 2(3H)-imino-1,3,4-thiadiazoles by oxidative cyclization of aldehyde thiosemicarbazones with Cu(II) or Fe(III) salts, a competitive reactivity study was performed on a suitable set of diversely substituted substrates, by means of HPLC techniques. This approach enabled to exploit Hammett’s equation without performing otherwise difficult-to-run kinetic experiments. The results presented herein support the hypothesis that the formation of the thiadiazole ring is induced by the attack of the oxidizing Lewis acid metal cation onto the imine-like nitrogen atom of the thiosemicarbazone substrate. Beyond mechanistic interpr…

Tieteelliset laskentasovellukset ja pilvipalvelut – erityistarkastelussa AWS

2014

Perinteisesti IT-resurssien hankinta on tapahtunut hankkimalla laitteistoa ja ohjelmistoja omaan tai organisaation omistukseen. Näiden resurssien käyttö on yleensä tarkoittanut merkittäviä investointeja laitteistoihin, ohjelmistoihin ja näiden ylläpitoon. Suuressa organisaatiossa kalliiden IT-resurssien käyttöönotto voi olla joissain tapauksissa hyvinkin byrokraattinen prosessi. Tieteellinen laskenta edellyttää usein erittäin suurta laskenta- ja tallennuskapasiteettia. Tutkijat hyötyisivät raskaaseen laskentaan vaadittavien IT-resurssien hankkimisesta palveluna, jolloin usein niukat resurssit voitaisiin keskittää vaadittavan laitteiston hankkimisen ja ylläpidon sijaan ydinongelman tutkimise…

Kazoo training for L2 pronunciation practice and reduced foreign accentedness?

2019

This paper presents a controlled pretest–training–posttest study on using a small membraphone instrument called kazoo for L2 pronunciation practice and reducing foreign accentedness. Learners were recorded for free speech before and after a six-week pronunciation and oral skills course including L2 prosody training with personal kazoos. A control group did not receive any kazoo training but did similar tasks in regular speech. Samples of all learners’ free speech before and after the course were rated for foreign accentedness by L1 speakers. In addition, learners taking part in the kazoo group were interviewed in focus groups to ascertain their views on kazoo training. The results imply tha…