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5-substituted analogues of 3-hydroxymethyl-5-aziridinyl-1-methyl-2-[1H-indole-4,7-dione]prop-2-en- 1-ol (EO9, NSC 382459) and their regioisomers as hypoxia-selective agents: structure-cytotoxicity in vitro.
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A series of regioisomeric analogues of 3-hydroxymethyl-5-aziridinyl-1-methyl-2-[1H-indole-4,7-dione]prop-2-en-1 -ol (EO9, NSC 382459) with the hydroxymethyl and hydroxypropenyl substituents situated at either the 2- or the 3-position of the indole ring were synthesized. The compound lacking the
Anoxia promotes gravitropic curvature in rice pulvini but inhibits it in wheat and oat pulvini.
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Gravitropic curvature of pulvini of wheat and oat stem segments gradually declined with decreasing atmospheric O₂ concentration and was almost completely blocked under anoxia, whereas that of rice stem segments was enhanced under hypoxia and anoxia. Anoxia substantially increased the ethanol content
Development of the new group of indole-derived neuroprotective drugs affecting oxidative stress.
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1. The role of oxidative stress, and accordingly uncontrolled reactive oxygen species generation/action, have been widely documented in a number of different neuronal pathologies. However, the concept of pharmacological interventions in prevention and therapy of oxidative stress-related diseases has
Indole conjugated silica and magnetic nanoparticles as inhibitors of HIF.
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Multifunctional silica nano-vehicles (SiO2@indol-IL) and magnetic nanoparticles (Fe3O4@indol-IL) were constructed through the Schiff bases condensation of indole-3-carboxaldehyde and 4-acetyl-N-allyl pyridinium chloride (ILs) with the amine groups of silica and magnetic nanoparticles. SiO2@indol-IL
Indole-3-carbinol is a potent inhibitor of ischemia-reperfusion-induced inflammation.
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BACKGROUND
Ischemia-reperfusion (I/R) induces tissue inflammation, which is characterized by an increased leukocyte-endothelial cell interaction and leukocyte transmigration. These processes are mediated by the activation of the nuclear factor (NF)κB signaling pathway, resulting in an elevated
Indole derivatives as neuroprotectants.
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It seems to be satisfactorily proved that reactive oxygen species (ROS) participate in numerous pathological processes in the nervous system (NS). Compounds able to interfere with the action of ROS might be useful in prevention and treatment of these pathologies. The search is focused on compounds
An Unsymmetrical Squaraine-based Activatable Probe for Imaging Lymphatic Metastasis through Responding to Tumor Hypoxia by MSOT and Aggregation-enhanced Fluorescent Imaging.
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Optoacoustic imaging exhibits great potential for preclinical research and clinical practice, and designing robust activatable optoacoustic probes for specific diseases is beneficial for its further development. Herein, an activatable probe has been developed for tumor hypoxia imaging. For this
[Antihypoxic and antiedemic activity of new condensed indole derivatives].
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The antihypoxic and antiedemic activity of a series of new indole derivatives and condensed systems, including pyrimido-, thiazolo-, and triazinoindoles, was studied on the hypobaric hypoxic hypoxia ad toxic lung edema models. Several thiazoloindole and formylindole derivatives prevented the loss of
Protective effect of thiazolo[5,4-b]indole in toxic pulmonary edema.
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Antiedematous activity of new thiazolo[5,4-b]indole derivatives containing a fragment of isothiourea and characterized by higher antihypoxic activity compared to known antihypoxants was studied on a model of toxic edema of the lungs in mice. Compounds exhibiting high activity on two models of
Novel chimeric gene promoters responsive to hypoxia and ionizing radiation.
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Despite being an adverse prognostic factor in radiotherapy, hypoxia represents a physiological difference that can be exploited for selective cancer gene therapy. In this study gene therapy vectors responsive to both hypoxia and ionizing radiation (IR) were developed. Gene expression was regulated
3,3'‑Diindolylmethane attenuates cardiomyocyte hypoxia by modulating autophagy in H9c2 cells.
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Autophagy is activated in the ischemic heart and is a process that is essential for survival, differentiation, development and homeostasis. 3,3'‑Diindolylmethane (DIM) is a natural product of the acid‑catalyzed condensation of indole‑3‑carbinol in cruciferous vegetables. Numerous studies have
Molecular targets, anti-cancer properties and potency of synthetic indole-3-carbinol derivatives.
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The indole-3-carbinol (I3C) displays anti-proliferative and anti-cancer activities against human cancer cells. Cellular proliferation is an important event associated with cancer development and continued progression. This manifest is described by altered expression and/or functions of cell cycle
Factors affecting sensitivity to EO9 in rodent and human tumour cells in vitro: DT-diaphorase activity and hypoxia.
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Twenty-three human tumour cell lines (lung, breast, and colon) and eight rodent cell lines were evaluated for their sensitivity to the quinone-based anticancer drug EO9 [3-hydroxymethyl-5-aziridinyl-1-methyl-2-(1H indole-4,7-dione)prop-beta-en-alpha-o1]. Sensitivity was compared with the
Uremia induces abnormal oxygen consumption in tubules and aggravates chronic hypoxia of the kidney via oxidative stress.
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In addition to causing uremic symptoms, uremic toxins accelerate the progression of renal failure. To elucidate the pathophysiology of uremic states, we investigated the effect of indoxyl sulfate (IS), a representative uremic toxin, on oxygen metabolism in tubular cells. We demonstrated an increase
A Tryptoline Ring-Distortion Strategy Leads to Complex and Diverse Biologically Active Molecules from the Indole Alkaloid Yohimbine.
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High-throughput screening (HTS) is the primary driver to current drug-discovery efforts. New therapeutic agents that enter the market are a direct reflection of the structurally simple compounds that make up screening libraries. Unlike medically relevant natural products (e.g., morphine), small
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