Search results for "Indole"
showing 10 items of 570 documents
Scandium-catalyzed preparation of cytotoxic 3-functionalized quinolin-2-ones: Regioselective ring enlargement of isatins or imino isatins
2012
Trimethylsilyldiazomethane in the presence of catalytic amounts of Sc(OTf) 3 smoothly promotes the ring expansion of isatins or imino isatins to efficiently afford 3-functionalized quinolin-2-ones through controlled ring enlargement. Whereas the ring-expansion reaction of azetidine-2,3-diones led to the adduct resulting from migration of the carbonyl group, the ring-expansion reaction of oxindole derivatives gave the adduct resulting from migration of the aryl group. To rationalize the experimental observations, theoretical studies have been performed. Moreover, the biological activity of some of the synthesized heterocycles has been evaluated in four cancer cell lines. © 2012 Wiley-VCH Ver…
Core‐shell nanoparticles with hyperbranched poly(arylene‐oxindole) interiors
2009
Opracowano synteze wysoce rozgalezionego poli(aryleno-oksyndolu) na drodze reakcji polimeryzacji pochodnej 5-bromoizatyny, a nastepnie modyfikacji terminalnych jednostek izatynowych. Tak przygotowany polimerowy rdzen, charakteryzujący sie stopniem rozgalezienia 100 %, byl substratem do rodnikowej polimeryzacji z przeniesieniem atomu (z ang. ATRP) w reakcji z akrylanem tert-butylu. Otrzymane kopolimery zawierające hydrofobowy rdzen i alkilowe lancuchy zakonczone wolnymi grupami karboksylowymi tworzą sferyczne nanocząstki. Przedstawiono wstepne wyniki badan dotyczących ich wlaściwości fizykochemicznych oraz potencjalnych zastosowan.
Comparison of the Effects of Indole-3-Acetic Acid and Kinetin on the Photosynthetic Apparatus and on the Cell Metabolism
1984
External and internal factors can exert a regulatory influence on growth and differentiation within a reaction norm determined by the genetic material. As to the internal factors, the phytohormones intervene in the most development processes in a regulatory manner. In a number of publications it was pointed out that there is a far-reaching accordance between the effects caused by I.4A and the effects induced by red light and low light conditions (Zerbe, Wild, 1980 a; Holzapfel et al., 1982 a). Plants of Sinapis alba grown under low light conditions but additionally treated with kinetin show changes in their metabolism that are characteristic of plants grown at higher light intensities (Zerb…
Closer Investigation of the Kinetics and Mechanism of Spirovinylcyclopropyl Oxindole Reaction with 3Σ–g-O2 by Topological Approaches and Unraveling t…
2021
In this investigation at the MN15L/Def2-TZVP level of theory, we present computational evidence indicating that the reaction of 3Σ-g-O2 with spirovinylcyclopropyl oxindole (2) leads to a product called spiro-1,2-dioxolane (2) in its singlet state; this reaction occurs via a stepwise mechanism and its rate-determining step is catalyzed by iodine radicals, which promotes opening of the three-membered ring under dark conditions. The conversion of 2 to 1-benzylindoline-2,3-dione (3) and 2-vinyloxirane (4) takes place via a concerted and slightly asynchronous reaction. Both electron localization function and AIM topological analysis reveal that the step associated with the attack of the 3Σ-g-O2 …
Organocatalytic Domino Oxa-Michael/1,6-Addition Reactions: Asymmetric Synthesis of Chromans Bearing Oxindole Scaffolds.
2016
An asymmetric organocatalytic domino oxa-Michael/1,6-addition reaction of ortho-hydroxyphenyl-substituted para-quinone methides and isatin-derived enoates has been developed. In the presence of 5 mol % of a bifunctional thiourea organocatalyst, this scalable domino reaction affords 4-phenyl-substituted chromans bearing spiro-connected oxindole scaffolds and three adjacent stereogenic centers in good to excellent yields (up to 98 %) and with very high stereoselectivities (up to >20:1 d.r., >99 % ee).
1-{3-[(7-Fluoro-9H-pyrimido[4,5-b]indol-4-yl)(methyl)amino]piperidin-1-yl}propan-1-one
2021
The title compound, C19H22FN5O, has been synthesized as an inhibitor of glycogen synthase kinase-3β. Two molecules interact via two N—H...N hydrogen bonds, forming centrosymmetric dimers.
Targeting the vascular endothelial growth factor system to prevent ovarian hyperstimulation syndrome
2008
BACKGROUND: Ovarian hyperstimulation syndrome (OHSS) typically occurs when ovaries are primed with FSH/ LH and subsequently exposed to hCG. The ultimate pathophysiological step underlying this clinical picture is increased vascular permeability (VP). METHODS: A search of the literature was carried out using PubMed and the authors’ files. RESULTS: In rodents and humans, the expression of vascular endothelial growth factor (VEGF) and VEGF receptor 2 (VEGFR-2) mRNA increases during ovarian stimulation. With the administration of hCG, the expression of each rises to a maximum. Expression of VEGF/VEGFR-2 mRNAs correlates with enhanced VP, with both peaking 48 h following an injection of hCG. Imm…
In vitro effects of estradiol, testosterone, and progesterone on 5-methoxyindole content, cyclic adenosine 3',5'-monophosphate synthesis, and norepin…
1986
To examine the effects of estradiol, testosterone, or progesterone on cyclic adenosine 3',5'-monophosphate (AMP) accumulation, 5-methoxyindole levels, and norepinephrine (NE) release by the female guinea pig pineal complex, samples of the deep, intermediate, or superficial portions of the complex were incubated in vitro with varied concentrations of either hormone. Exposure for 10 minutes to physiological amounts of estradiol (10 nM) or to 100 microM NE increased significantly cyclic AMP levels to the same extent in the three pineal regions. A maximal effect on cyclic AMP accumulation was observed at 100-nM concentrations of estradiol, with a tendency to return to basal levels at 1-10 micro…
Transgenic overexpression of corticotropin releasing hormone provides partial protection against neurodegeneration in an in vivo model of acute excit…
2008
Abstract Corticotropin releasing hormone (CRH) is the central modulator of the mammalian hypothalamic–pituitary–adrenal (HPA) axis. In addition, CRH affects other processes in the brain including learning, memory, and synaptic plasticity. Moreover, CRH has been shown to play a role in nerve cell survival under apoptotic conditions and to serve as an endogenous neuroprotectant in vitro . Employing mice overexpressing murine CRH in the CNS, we observed a differential response of CRH-overexpressing mice (CRH-COE hom -Nes) to acute excitotoxic stress induced by kainate compared with controls (CRH-COE con -Nes). Interestingly, CRH-overexpression reduced the duration of epileptic seizures and pre…
Evaluation of PAI-1 in endometriosis using a homologous immunocompetent mouse model
2018
To analyze the role of PAI-1 (plasminogen activator inhibitor 1) in endometriotic lesion growth, we studied the effect of PAI-1 inhibition by PAI-039 using a homologous mouse model of endometriosis that allows noninvasive monitoring. Endometrial tissue from donor mice was collected, labeled with mCherry adenovirus, and implanted into a subcutaneous pocket on the ventral abdomen of recipient mice. Seven days after transplantation, mice were randomly allocated in two groups and treated once daily for 2 weeks with either vehicle (control group) or PAI-1 inhibitor (PAI-039 group). Endometriotic lesion size generated in recipient mice was monitored by mCherry signal. Animals were euthanized 21 d…