Academic literature on the topic 'Indolinoren'

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Journal articles on the topic "Indolinoren"

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Anna, Markina, and Mishсhenko Oksana. "The influence of indolinoren on kidney function in conditions of water and salt load." ScienceRise: Pharmaceutical Science, no. 4(14) (August 31, 2018): 20–23. https://doi.org/10.15587/2519-4852.2018.141304.

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Diuretics are widely used to correct kidney disorders. In turn, the ionic composition of food, mostly sodium ions, which directly affect the excretory function of the kidneys, can act as modulators of the action of diuretics. The aim of the study was to investigate the effects of the new 2-oxoindoline derivative with the conventional name "Indolinoren" on the state of the excretory function of the kidneys under the conditions of water and salt load. Materials and methods. Studies were performed on white non-linear rats. The water load was modelled by introducing distilled water (5 ml per 100 g of body weight of the animal); salt load - intragastric administration of 0.45 % sodium chloride solution in an amount of 3 % of body weight. Indolinoren and comparison drug furosemide were administered intragastrically at a dose of 29.5 mg / kg and 5 mg / kg, respectively. Results and discussion. It has been established that indolinoren has a saluretic effect in conditions of water load, accompanied by an increase in sodium excretion by 132 % and potassium by 2.4 %. Against the background of the introduction of indolinoren, a significant increase in the sodium-potassium coefficient of urine was established 2.3-fold (p <0.05), which indicates a more pronounced natriuresis than kaliuresis. Under conditions of salt load, indolinoren promotes a significant increase in urine output by 381 % (p <0.05), increases sodium excretion by 127 % (p <0.05), potassium by 7 %. There were no significant differences in creatinine excretion. The expression of diuretic activity in conditions of salt load indolinoren exceeds furosemide and does not have a significant difference under conditions of water load. Conclusion: The increase in natriuresis and, to a lesser extent, the kaliuresis, as well as the absence of significant changes in the excretion of creatinine, a glomerular filtration marker, on the background of the introduction of indolinoren indicates that its diuretic effect is realized due to oppression of tubular reabsorption. In the mechanism of indolinoren action involved inhibition of mineralocorticoid control of the excretory function of the kidney, as evidenced by the increase in the sodium-potassium coefficient of urine. The obtained data justify the need for further in-depth study of indolinoren as a perspective diuretic
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Markina, A. Yu, and O. Ya Mishchenko. "The experimental study of antihypoxic and antioxidant indolinoren activity." Ukraïns’kij bìofarmacevtičnij žurnal, no. 3(50) (June 16, 2017): 22–25. http://dx.doi.org/10.24959/ubphj.17.112.

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Chakrabarty, Manas, Sandipan Sarkar, and Yoshihiro Harigaya. "A Facile Clay-Mediated Synthesis of 3,3-diindolyl-2-indolinones from Isatins." Journal of Chemical Research 2005, no. 8 (2005): 540–42. http://dx.doi.org/10.3184/030823405774663264.

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Dry reaction of isatins (3a, 3b) with indoles (4a–e) on montmorillonite K10 clay at room temperature furnished within minutes 3,3-bis(3′-indolyl)-2-indolinones (1a–f) in high yields. 5-Nitroisatin (3c) furnished, in addition to the expected indolinone 1h, 3-hydroxy-3-(3′-indolyl)-5-nitro-2-indolinone (6), a likely intermediate to 1h.
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Markina, Anna, and Oksana Mishсhenko. "The influence of indolinoren on kidney function in conditions of water and salt load." ScienceRise: Pharmaceutical Science, no. 4 (14) (August 31, 2018): 20–23. http://dx.doi.org/10.15587/2519-4852.2018.141304.

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Markina, Anna, Oksana Mishсhenko, and Julia Laryanovska. "The impact of indolinoren on histrotructure of kidney on the glixerroid acute renal failure model." ScienceRise: Pharmaceutical Science, no. 5 (9) (October 31, 2017): 10–14. http://dx.doi.org/10.15587/2519-4852.2017.113361.

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B., Raja Sekhara Reddy, Reddy P. Malleswara, Babu G. Surendra, Narayana V. Venkata, and Babu K. Sudhakar. "Organo catalytic construction of novel Pyrazol-2-Indolinone derivatives." Research Journal of Chemistry and Environment 26, no. 2 (2022): 9–13. http://dx.doi.org/10.25303/2602rjce0913.

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A few novel series of pyrazol-2-indolinone entities have been designed and synthesized using pyrazalone and α, β-unsaturated oxindole esters as starting materials (5a–j). The chemical structures of the new synthesized compounds were characterized by 1H NMR, 13C NMR, MS spectroscopy and elemental analysis. This procedure provides a highly efficient and facile route to functionalized pyrazol-2-indolinones from readily available substrates under mild reaction conditions.
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Smallheer, J. M., M. J. Otto, C. A. Amaral-Ly, et al. "Synthesis and anti-HIV Activity of a Series of 2-Indolinones and Related Analogues." Antiviral Chemistry and Chemotherapy 4, no. 1 (1993): 27–39. http://dx.doi.org/10.1177/095632029300400104.

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A novel series of 2-indolinones with in vitro anti-HIV (human immunodeficiency virus) activity is described. Two structurally related compounds, 1, 3,3-(4- N-methyl-1,2,5,6-tetrahydropyridylmethyl)-1- phenyl-2-indolinone, and 2, its 4- N-methylpiperidinylmethyl analogue (Fig. 1), formed the basis of a structure-activity study. The synthesis of approximately 50 analogues and their respective activities vs. HIV are presented. Both 1 and 2 were effective inhibitors of HIV(IIIb) in cell protection assays with IC90 values of 4.4 and 14.9μM (2.2 and 7.9μg ml−1), respectively. In the same concentration range, 1 and 2 also inhibit syncytia formation. These compounds represent a novel class of anti-HIV agents which appear to act by inhibiting virus-dependent cell fusion.
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Liao, Albert T., May B. Chien, Narmada Shenoy, et al. "Inhibition of constitutively active forms of mutant kit by multitargeted indolinone tyrosine kinase inhibitors." Blood 100, no. 2 (2002): 585–93. http://dx.doi.org/10.1182/blood-2001-12-0350.

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Abstract Mutations in the proto-oncogene c-kit, including point mutations, deletions, or duplications in the negative regulatory juxtamembrane (JM) domain or point mutations in the catalytic domain, have been observed in human and canine cancers and often result in constitutive activation of Kit in the absence of ligand binding. To identify a receptor tyrosine kinase (RTK) inhibitor capable of blocking the function of mutant Kit, we evaluated 3 indolinones (SU11652, SU11654, and SU11655) that act as competitive inhibitors of adenosine triphosphate binding to several members of the split kinase family of RTKs, including VEGFR, FGFR, PDGFR, and Kit. Mast cell lines expressing either wild-type (WT) Kit, a point mutation in the JM domain, a tandem duplication in the JM domain, or a point mutation in the catalytic domain were used for these studies. All 3 indolinones inhibited phosphorylation of WT Kit in the presence of stem cell factor at concentrations as low as 0.01 μM. Autophosphorylation of both JM mutants was inhibited at 0.01 to 0.1 μM, resulting in cell cycle arrest within 24 hours, whereas autophosphorylation of the catalytic domain mutant was inhibited at 0.25 to 0.5 μM, resulting in cell death within 24 hours. poly(ADP-ribose) polymerase (PARP) cleavage was noted in all Kit mutant lines after indolinone treatment. In summary, SU11652, SU11654, and SU11655 are effective RTK inhibitors capable of disrupting the function of all forms of mutant Kit. Because the concentrations of drug necessary for receptor inhibition are readily achievable and nontoxic in vivo, these compounds may be useful in the treatment of spontaneous cancers expressing Kit mutations.
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Somogyi, László, and Attila Csaba Bényei. "Contributions to the chemistry of 3-cyanoacetylhydrazono-2-indolinones and X-ray structure ofZ-3-cyanoacetylhydrazono-2-indolinone monohydrate." Heteroatom Chemistry 20, no. 4 (2009): 183–93. http://dx.doi.org/10.1002/hc.20531.

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Ivanenkov, Yan A., Maxim E. Kukushkin, Anastasia A. Beloglazkina, et al. "Synthesis and Biological Evaluation of Novel Dispiro-Indolinones with Anticancer Activity." Molecules 28, no. 3 (2023): 1325. http://dx.doi.org/10.3390/molecules28031325.

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Novel variously substituted thiohydantoin-based dispiro-indolinones were prepared using a regio- and diastereoselective synthetic route from 5-arylidene-2-thiohydantoins, isatines, and sarcosine. The obtained molecules were subsequently evaluated in vitro against the cancer cell lines LNCaP, PC3, HCTwt, and HCT(−/−). Several compounds demonstrated a relatively high cytotoxic activity vs. LNCaP cells (IC50 = 1.2–3.5 µM) and a reasonable selectivity index (SI = 3–10). Confocal microscopy revealed that the conjugate of propargyl-substituted dispiro-indolinone with the fluorescent dye Sulfo-Cy5-azide was mainly localized in the cytoplasm of HEK293 cells. P388-inoculated mice and HCT116-xenograft BALB/c nude mice were used to evaluate the anticancer activity of compound 29 in vivo. Particularly, the TGRI value for the P388 model was 93% at the final control timepoint. No mortality was registered among the population up to day 31 of the study. In the HCT116 xenograft model, the compound (170 mg/kg, i.p., o.d., 10 days) provided a T/C ratio close to 60% on day 8 after the treatment was completed. The therapeutic index—estimated as LD50/ED50—for compound 29 in mice was ≥2.5. Molecular docking studies were carried out to predict the possible binding modes of the examined molecules towards MDM2 as the feasible biological target. However, such a mechanism was not confirmed by Western blot data and, apparently, the synthesized compounds have a different mechanism of cytotoxic action.
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Dissertations / Theses on the topic "Indolinoren"

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Cox, Kaleb Woodrow. "Synthesis and Biological Activity of Indolinones." Wright State University / OhioLINK, 2014. http://rave.ohiolink.edu/etdc/view?acc_num=wright1421165680.

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Lumetzberger, Astrid. "Potentielle VEGFR- und EGFR- Tyrosinkinase-Inhibitoren des 2-Indolinon- und des 4-Anilinochinazolin-Typs." [S.l.] : [s.n.], 2004. http://www.diss.fu-berlin.de/2004/152/index.html.

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Simon, Ingrid. "Indolo[2,3-b]quinoléines : cascade radicalaire combinant une cyclisation 5-exo-trig avec le réarrangement de Smiles." Thesis, Reims, 2013. http://www.theses.fr/2013REIMP203/document.

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Le squelette indolo[2,3-b]quinoléique est une cible synthétique attrayante car il est présent notamment dans la néocryptolépine, alcaloïde aux propriétés cytotoxiques et antipaludéennes. Nous proposons ici une approche originale pour accéder à ce tétracycle, qui combine dans une réaction radicalaire en cascade une cyclisation à un réarrangement de Smiles. La mise au point des conditions expérimentales et l'étude mécanistique de cette voie ont constitué le premier objectif de ce travail. Outre les produits attendus, les études structurales approfondies ont mis en évidence la formation de composés inédits résultant d'étapes radicalaires supplémentaires. En parallèle, l'application de la méthode à un substrat judicieusement fonctionnalisé a conduit au 3-(2'-aryl-N-alkylacétamido)oxindole, un intermédiaire clé vers le système indolo[2,3-b]quinoléique 6 et 11 disubstitué ciblé<br>The indolo[2,3-b]quinoline ring system is an attractive synthetic target present in neocryptolepine, an antiplasmodial and cytotoxic alkaloid. We proposed an original pathway toward this squeleton, combining as key step a 5-exo-trig cyclisation to a Smiles rearrangement in a domino radical process. We first focused on scope and limitations studies and mechanistic investigations. Apart from the cyclised-rearranged products we isolated new original structures resulting from supplementary radical reactions. The application of the developed method to a conveniently functionalised substrate led to 3-(2'-aryl-N-alkylacetamido)indolinone, a key intermediate which was further converted to the aimed 6,11-disubstituted indolo[2,3-b]quinoline tetracycle
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Rosen, Joachim. "Vergleich der Radikalreaktionen von Melatonin und strukturverwandten Indolaminen in unterschiedlichen Oxidationssystemen." Doctoral thesis, 2006. http://hdl.handle.net/11858/00-1735-0000-0006-B616-2.

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Lumetzberger, Astrid [Verfasser]. "Potentielle VEGFR- und EGFR- Tyrosinkinase-Inhibitoren des 2-Indolinon- und des 4-Anilinochinazolin-Typs / vorgelegt von Astrid Lumetzberger." 2004. http://d-nb.info/971640149/34.

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Books on the topic "Indolinoren"

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Maass, Gerhard. Charakterisierung der Thiazolo-iso-indolinone, einer neuen Klasse nichtnukleosidischer Inhibitoren der Reversen Transkriptase von HIV-1. 1993.

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Book chapters on the topic "Indolinoren"

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"2′,3-Biindolinylidene-2,3′-dione: 3-(3-Indolinone-2-ylidene)-indolin-2-one." In Encyclopedia of Cancer. Springer Berlin Heidelberg, 2017. http://dx.doi.org/10.1007/978-3-662-46875-3_100022.

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Conference papers on the topic "Indolinoren"

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Bruni, Paolo, Eziana Maurelli, and Giorgio Tosi. "Association and solvation of indolinones." In Fourier Transform Spectroscopy: Ninth International Conference, edited by John E. Bertie and Hal Wieser. SPIE, 1994. http://dx.doi.org/10.1117/12.166740.

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