Search results for "Anilide"
showing 10 items of 40 documents
Apoptosis induced in HepG2 cells by the synthetic cannabinoid WIN: involvement of the transcription factor PPARgamma.
2008
It has recently been shown that cannabinoids induce growth inhibition and apoptosis in different tumour cell lines. In the current study, the effects of WIN 55,212-2 (WIN), a synthetic and potent cannabinoid receptor agonist, are investigated in hepatoma HepG2 cells and a possible signal transduction pathway is proposed. In these cells, WIN induces a clear apoptotic effect which was accompanied by up-regulation of the death-signalling factors Bax, Bcl-X(S), t-Bid and down-regulation of the survival factors survivin, phospho-AKT, Hsp72 and Bcl-2. Moreover, WIN-induced apoptosis is associated with JNK/p38 MAPK pathway activation and mitochondrial depolarisation demonstrated by a cytofluorimet…
Cemiplimab in locally advanced basal cell carcinoma after hedgehog inhibitor therapy: an open-label, multi-centre, single-arm, phase 2 trial.
2021
Summary Background Before February, 2021, there was no standard treatment regimen for locally advanced basal cell carcinoma after first-line hedgehog inhibitor (HHI) therapy. Cemiplimab, a PD-1 antibody, is approved for treatment of advanced cutaneous squamous cell carcinoma and has shown clinical activity as monotherapy in first-line non-small-cell lung cancer. Here, we present the primary analysis data of cemiplimab in patients with locally advanced basal cell carcinoma after HHI therapy. Methods We did an open-label, multicentre, single-arm, phase 2 trial across 38 outpatient clinics, primarily at academic medical centres, in Canada, Europe, and the USA. Eligible patients (aged ≥18 years…
ortho-Substituent effects inN-arylacetamides. NMR and molecular mechanics investigation
1995
1H, 13C, 15N and 17O NMR spectra of N-phenylacetamide (acetanilide) and 21 ortho-substituted acetanilides were measured and assigned. The observed NMR parameters are related to the Hammett substituent parameters and conformational characteristics of the acetamido moiety estimated by molecular mechanics calculations. Significant relationships were found for the 13C NMR chemical shifts of C-5 (para to substituent) and the direct spin–spin coupling constant, 1J(C, H), of C-3 (ortho to substituent) with Hammett substituent parameters. For 15N NMR chemical shifts of the amido nitrogen, no general correlation with the Hammett substituent parameters was found. The interactions between functionalit…
Safety and efficacy of ombitasvir/paritaprevir/ritonavir/dasabuvir plus ribavirin in patients over 65 years with HCV genotype 1 cirrhosis
2018
Purpose: To analyse safety and efficacy of treatment based on ombitasvir/paritaprevir/ritonavir/dasabuvir plus ribavirin in the sub-group of GT1 patients older than 65 years. Methods: We collected data extracted from the ABACUS compassionate-use nationwide Italian programme, in patients with cirrhosis due to hepatitis C virus (HCV) Genotype-1 (GT1) or 4 and at high risk of decompensation. GT1-HCV-infected patients received once-daily ombitasvir/paritaprevir, with the pharmacokinetic enhancer ritonavir (25/150/100 mg) and twice-daily dasabuvir (250 mg) plus Ribavirin (RBV) (OBV/PTV/r + DSV + RBV) for 12 (GT1b) or 24 (GT1a) weeks. Endpoints were to evaluate safety and efficacy, the latter def…
Hsp60 Inhibitors and Modulators
2019
In this chapter, we focus on the 60 KDa Heat Shock Protein (Hsp60) and discuss some of its biological, molecular and pathological features. The structural and mechanistic aspect of the Hsp60 folding cycle will be also presented. We further illustrate how Hsp60 may be involved in many diseases and therefore considered as an effective therapeutic or theranostic target. Finally, the state-of-the-art on the development of Hsp60 and bacterial GroEL inhibitors and modulators of their expression will be illustrated. This is discussed in the light of a negative chaperonotherapy, and the consequent development of inhibitors, as well as positive chaperonotherapy, in the event its excessive activity i…
Lower Urinary Tract Symptoms: What's New in Medical Treatment?
2018
Abstract Context Pharmacological treatment is a cornerstone in the management of patients with lower urinary tract symptoms (LUTS). Objective To review emerging evidence in the medical treatment of LUTS. Evidence acquisition An Embase/Pubmed-based literature search was conducted in December 2017, screening for randomized controlled trials (RCTs), prospective and retrospective series, animal model studies, and reviews on medical treatment of LUTS. Evidence synthesis The main medical innovation in recent years in overactive bladder (OAB) has been the approval of the first β 3 -adrenoceptor agonists (mirabegron) and intradetrusor onabotulinum toxin A, while several other drugs such as antiepil…
Virtual Combinatorial Syntheses and Computational Screening of New Potential Anti-Herpes Compounds
1999
The activity of new anti-HSV-1 chemical structures, designed by virtual combinatorial chemical synthesis and selected by a computational screening, is determined by an in vitro assay. A virtual library of phenol esters and anilides was formed from two databases of building blocks: one with carbonyl fragments and the other containing both substituted phenoxy and phenylamino fragments. The library of virtually assembled compounds was computationally screened, and those compounds which were selected by our mathematical model as active ones were finally synthesized and tested. Our antiviral activity model is a "tandem" of four linear functions of topological graph-theoretical descriptors. A giv…
A randomized trial comparing tamoxifen therapy vs. tamoxifen prophylaxis in bicalutamide-induced gynecomastia.
2012
BACKGROUND: Tamoxifen (TAM) has been shown to be active against the bicalutamide-induced breast events (BEs) gynecomastia, and breast pain in patients with prostate cancer (PC). Optimal doses and schedules are not yet established. Debate still exists about whether prophylaxis with TAM is more effective than treatment of BEs when diagnosed. The results of a randomized study comparing TAM prophylaxis vs. TAM therapy are presented. METHODS: One hundred seventy-six patients with prostate cancer (PC) who were candidates for bicalutamide monotherapy were randomized to receive TAM 20 mg daily orally within 1 month from the onset of BEs (arm A) vs. TAM 10 mg daily starting simultaneously with bical…
Studies in organic mass spectrometry. Part 23. Role of the aroyl group on the competitive fragmentation reactions of the molecular ion of aroylanilid…
1999
The 70 eV and mass-analysed ion kinetic energy (MIKE) spectra of some thiophenecarboxanilides and benzoylanilides (1–10) have been compared in order to investigate the role of the aroyl (or heteroaroyl) moiety on the abundance of the competitive fragmentation reactions occurring in their molecular ions (amide–bond cleavage and phenol radical ion formation). It has been shown that the electron ionisation induced decompositions with high (70 eV) and low (MIKE) internal energy excess are qualitatively similar, but remarkable quantitative differences have been observed that can be accounted for in terms of the different effectiveness in the transmission of electronic effects of substituents in …
Studies in organic mass spectrometry. Part 20: a hidden ortho effect in the electron ionisation mass spectra of some 2′-alkyl substituted 2-and 3-thi…
1996
The electron-ionisation-induced amide-bond cleavage of some 2′-methyl- and 2′-ethyl-substituted 2- and 3-thiophenecarboxanilides, which yields formally anilylium ions having relative intensities apparently in contrast with the Stevenson‐Audier rule, has been investigated by mass-analysed ion kinetic energy (MIKE) spectrometry and compared to that of the 3 ′- and 4′-isomers. It has been shown that, in the case of the 2 ′-methyl and 2′-ethyl derivatives, the amide-bond cleavage is anchimerically assisted through the hidden migration of a benzyl hydrogen to the nitrogen. Analysis of the MIKE and collision-induced decomposition (CID) MIKE spectra of model compounds indicates that this cryptic o…