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Analysis of Table shows that compound
2020-06-20
Analysis of Table 1 shows that compound 7b, in which the biphenyl scaffold does not bear any substituent, displays its inhibitory potency in the micromolar range (IC50 = 11 μM). If the amide bridge is moved from position 1 to 3 of the biphenyl system, product 7c is yielded, whose potency is about 4
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DBU As for antiviral activity eight
2020-06-20
As for antiviral activity, eight out of 23 synthesized compounds were active against influenza B virus with EC50 values in the range of 0.19–39 μM. Four of the eight influenza B hits were active against influenza A and two were also active against RSV (4 and 6, EC50 = 0.40 and 1.8 μM, respectively).
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Cryptosporidium is a protist causing serious diarrhea in hum
2020-06-20
Cryptosporidium is a protist causing serious diarrhea in humans and other animals (Bouzid et al. 2013). In its mitosomes, the most reduced forms of mitochondria, it is assumed that the membrane potential is generated by a simple respiratory chain consisting of transhydrogenase, type II NADH dehydrog
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Besides degrading cholesterol the cholesterol degradation pa
2020-06-20
Besides degrading cholesterol, the cholesterol degradation pathway also offers a route to obtain useful starting materials for the production of steroid drugs and hormones. Indeed, steroids are among the most marketed pharmaceuticals with about 300 approved steroid drugs [15] and a worldwide market
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Previously we have shown that complexes of protein PKs
2020-06-19
Previously, we have shown that complexes of protein PKs with inhibitors that comprised sulfur or selenium atoms in aromatic structures were phosphorescent at room temperature, while the long-lifetime signal emitted by the free inhibitor was negligible.34, 35, 36 This phenomenon was caused by stabili
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ORY-1001 Introduction Cysteinyl leukotrienes CysLTs LTC LTD
2020-06-19
Introduction Cysteinyl leukotrienes (CysLTs), LTC4, LTD4 and LTE4, are 5-lipoxygenase pathway metabolites of arachidonic ORY-1001 and deeply involved in bronchial asthma via activation of CysLT1 receptors [1], [2]. Specific CysLT1 receptor antagonists, including pranlukast [3], [4] and montelukast
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Although information regarding the influence of PGE on cardi
2020-06-19
Although information regarding the influence of PGE2 on cardiac fibroblast cell growth is sparse, the effect of PGE2 on other cell types has been studied extensively, particularly in cancer and cancer cell lines where COX-2 is over-expressed. Constitutive high levels of COX-2 expression have been no
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As illustrated in Table monocyclic acid analogs
2020-06-19
As illustrated in Table 3, monocyclic Evans Blue tetrasodium salt analogs were synthesized and evaluated. 2-Oxido-3H-1,2,3,5-oxathiadiazol analog 8 showed 15-fold less potent EP1 receptor affinity relative to 2b, while it showed 2.2-fold more potent antagonist activity. Oxadiazole-5-one analog 9 ex
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Abdominal aortic aneurysm AAA is
2020-06-19
Abdominal aortic aneurysm (AAA) is considered a major health concern and is associated with extremely high rates of mortality in case of aortic rupture. The main pathophysiologic mechanisms leading to aortic dilation include the degradation of the extracellular matrix (ECM) components, such as colla
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cotransport In general cellular senescence is considered a p
2020-06-19
In general, cellular senescence is considered a programmed response to stress that can be activated by oxidative stress, irradiation or action of substances or drugs. These stressors cause DNA damage and, through the action of specific proteins (p53 and p21), lead to cell senescence (di Fagagna, 200
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To study the role of
2020-06-19
To study the role of DNA–PK in the response to replication arrest, we used the DNA replication inhibitor aphidicolin (APH). APH, a mycotoxin isolated from Cephalosporium aphidicola, inhibits DNA replication by interacting with the replicating DNA polymerase α (pol α). APH specifically inhibits the a
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Compound was generated using a literature procedure and
2020-06-19
Compound was generated using a literature procedure and required two-step Dess–Martin-periodinane/Pinnick oxidation prior to the methylation of the sulfonamide. Compound () was obtained from the Suzuki coupling of the methyl ester intermediate (en route to angiotensin 2 receptor blocker ). Hydro
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The N B method has the overall advantage that
2020-06-19
The N&B method has the overall advantage that it is not restricted to certain dyes specific for energy transfer [55], and is also able to detect higher order receptor Cy5 NHS ester on the focal point in living cells. Conclusion The N&B method has shown to be a powerful tool to locate and quantif
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br Introduction The cervix is a
2020-06-19
Introduction The GSA 10 australia is a poorly studied component of the mare’s reproductive tract. It has anatomical and biological defense mechanisms involved in the delicate balance between immunological tolerance, sperm transport and biological defense. Anatomically, the cervix is composed of
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In this work we fabricated a kind of multifunctional
2020-06-19
In this work, we fabricated a kind of multifunctional nanoparticles, based on HAuNS coated by chitosan-stearic Pyridoxal 5 phosphate copolymer (CSO-SA), which was employed frequently to form micelles for hydrophobic drug delivery in our previous work [21], [22]. The nanoparticles can encapsulate Di
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