A nickel-catalyzed decarbonylation or decarbonylation accompanied by decarboxylation cross-coupling reaction of aryl anhydrides with thiophenols as coupling partners was disclosed. This method is promoted by a commercially available, moisture-stable, and inexpensive nickel(II) precatalyst. The process can tolerate a variety of functional groups using ubiquitous aryl anhydrides as cross-coupling precursors to produce thioethers in moderate to excellent yields.
Bradykinin (BK) is an important mediator in several inflammatory and vascular diseases that acts in part via induction of cyclooxygenase-2 (COX-2). The mechanisms involved in BK-mediated COX-2 induction are unclear.Here we characterized the transcriptional mechanisms involved in human pulmonary artery smooth muscle cells. BK stimulated the activity of a transiently transfected 966-bp (؊917 to ؉ 49) COX-2 promoter luciferase reporter construct. There was no reduction in BK-induced luciferase activity in cells transfected with COX-2 promoter constructs of 674, 407, 239, and 135 bp or constructs with mutated CCAAT/enhancer-binding proteinor NF-B-binding sites. In contrast luciferase activity was reduced in cells transfected with a 407-bp COX-2 promoter fragment containing a mutated cAMP response element (CRE)-binding site, suggesting that the CRE binding site is critical. Electrophoretic mobility shift assays using oligonucleotides specific for the CREbinding region of the COX-2 promoter and consensus oligonucleotides showed strong specific binding. Furthermore BK increased consensus cAMP-responsive luciferase reporter (p6CRE/luc)-mediated luciferase expression. CRE activation occurred by BK inducing cytosolic phospholipase A 2 -mediated arachidonic acid release and rapid prostaglandin E 2 (PGE 2 ) production, thereby increasing cAMP. Indomethacin inhibited BKinduced PGE 2 production, cAMP accumulation, and CRE/luc reporter and COX-2 promoter luciferase activity. Exogenous PGE 2 and EP2 (ONO-AE1 259) and EP4 (ONO-AE1 329) PGE 2 receptor agonists mimicked the effect of BK. Collectively these studies indicate that COX-2 induction by BK in human pulmonary artery smooth muscle cells is mediated by the CRE through a novel autocrine loop involving endogenous PGE 2 .
A novel palladium-catalyzed three-component reaction for the synthesis of quinazolin-4(3H)-ones from readily available 2-aminobenzamides and aryl halides via a palladium-catalyzed isocyanide insertion/cyclization sequence has been developed. This methodology efficiently constructs quinazolin-4(3H)-ones in moderate to excellent yields with the advantages of operational simplicity.
A novel and highly efficient strategy for the synthesis of isocoumarins and phthalides through a palladium(0)-catalyzed reaction incorporating tert-butyl isocyanide has been developed. This process, providing one of the simplest methods for the synthesis of this class of valuable lactones, involves two steps including cyclization reaction and simple acid hydrolysis. The methodology is tolerant of a wide range of substrates and applicable to library synthesis.
Consumers, nowadays, are becoming mindful of environmental issues than ever. The rising concerns for the adverse effects of consumption on environmental sustainability are leading to transformation in consumer behaviour. Consumers need relevant sustainability information about the products to shape sustainable purchase behaviours. On this note, marketers and organizations are increasingly using labels and logos for integrating sustainability evidence in their product offerings. This research integrates the theory of planned behaviour (TPB) with environmental concern, consumer effectiveness, consumer innovativeness and sustainable label awareness to determine how these affect the sustainable purchase behaviour for food products in China. The findings of structural equation modelling using data gathered from 273 consumers indicate all the constructs as significant, with consumer innovativeness having a negative and significant association. The present research expects to contribute to advancement in the literature on TPB and sustainable labelling by presenting a comprehensive and distinct model. Given the importance of the factors highlighted in the current research, marketers can design appropriate strategies by leveraging these determinants. The outcomes imply that marketers and policymakers need to make the consumers aware of sustainable labels and their favourable effects on the environment to promote sustainable consumer behaviour.
Summary The p53 gene is a growth control gene, abnormalities of which have been implicated in a variety of cancers. Recently wild-type p53 has been shown to exist in two interchangeable conformational variants, which can be distinguished by specific p53 monoclonal antibodies. One conformation acts as a suppressor (PAb240-/PAbl620+) and one acts as a promoter (PAb240+/PAbl620-) of cell proliferation; the latter conformation is also that of mutant p53. We have previously shown that acute myeloblastic leukaemia (AML) blasts which proliferate autonomously in vitro express only p53 in the promoter conformation. In contrast, expression of PAb 1620 was found only in blasts with non-autocrine growth in vitro and was diminished following stimulation by exogenous growth factors when there was a switch to p53 in the promoter (PAb240+) conformation. As AML blasts with non-autocrine growth undergo apoptosis when deprived of exogenous growth factors, we studied whether this was mediated by wild-type p53. Antisense oligonucleotides to p53 were used to suppress p53 protein expression in blasts with non-autocrine growth and also the factor-dependent human erythroleukaemia cell line TF-1. Following growth factor deprivation for 48 h, 20.6-53.6% of control blasts were apoptotic and demonstrated a typical 'ladder' on DNA electrophoresis characteristic of internucleosomal degradation of DNA. In the presence of p53 antisense, apoptosis was suppressed despite the absence of growth factor, however cell proliferation was not stimulated. We conclude that apoptosis occurring in factor-dependent AML blasts following growth factor deprivation is mediated by wild-type p53 (PAb 1620+), and that conformational change of p53 to the PAb240+ conformation occurring either by mutation or by the action of autocrine growth factors would permit leukaemic cell survival by suppressing apoptosis.
A novel palladium-catalyzed formylation of aryl halides with isocyanide in the presence of Et3SiH has been demonstrated, which provides a strategy toward important aldehydes with moderate to excellent yield. The advantage of this reaction includes milder conditions, convenient operation, lower toxicity, and wide functional group tolerance.
A simple and highly efficient strategy for the synthesis of 3-substituted isocoumarins through a copper(I)-catalyzed reaction of 1-(2-halophenyl)-1,3-diones has been developed. The procedure is based on a cascade copper-catalyzed intramolecular Ullmann-type C-arylation and rearrangement process. This methodology is tolerant of a wide range of substrates and applicable to library synthesis.
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