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114618
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Showing 1-30 of 79 results for "114618" within Papers
Organic letters, 15(6), 1186-1189 (2013-03-07)
A facile method utilizing RCOX/K2CO3 as a novel reagent for conjugate addition of hydrogen halide, in addition to tertiary (3°)-hydroxyl protection that leads to the synthesis of functionalized β-halo Morita-Baylis-Hillman ester appended oxindoles, has been developed. The diastereoselective one-pot O-acylation-hydrohalogenation
Stress (Amsterdam, Netherlands), 8(3), 175-183 (2005-10-21)
(Indoledione 2,3) isatin is an endogenous indole found both in mammalian brain and peripheral tissues. Isatin concentration in blood can exceed 1 microM and tissue concentrations vary from < 0.1 to 10 microM. Its level in the brain and periphery
Identification and further development of thiazolidinones spiro-fused to indolin-2-ones as potent and selective inhibitors of Mycobacterium tuberculosis protein tyrosine phosphatase B
Tetrahedron, 67, 6713-6729 (2011)
Organic & biomolecular chemistry, 10(41), 8236-8243 (2012-09-15)
Yb(NTf(2))(3)-catalyzed [3 + 3] cycloaddition between isatin ketonitrones and cyclopropanes is described. A variety of spiro[tetrahydro-1,2-oxazine]oxindoles were obtained in moderate to good yields along with good regioselectivities. This is the first example of the intermolecular [3 + 3] cycloaddition between
Thiosemicarbazones: inhibition of the growth of pox viruses and requirement for the growth of an isatin-beta-thiosemicarbazone dependent mutant.
Reviews in clinical & basic pharmacology, 6(2), 119-130 (1987-04-01)
International journal of biological macromolecules, 155, 795-804 (2020-04-02)
An isatin functionalized chitosan derived ion-imprinted adsorbent (Cu-CIS) was designed by tailoring Cu(II) ions imprinted cavities within the modified polysaccharide network matrix that are able to capture Cu(II) ions selectively in aqueous solution. The chelating power of chitosan toward the
Novel Synthesis of Some Phthalazinone Derivatives
Chin. J. Chem., 29, 1446-1450 (2011)
Bioorganic & medicinal chemistry letters, 20(22), 6479-6482 (2010-10-12)
A series of N-substituted-3-[(2'-hydroxy-4'-prenyloxy)-phenyl]-5-phenyl-4,5-dihydro-(1H)-pyrazolines were synthesized and tested on human monoamine oxidase-A and -B isoforms. Structure-activity relationships and molecular modelling showed that some substitutions, such as benzyloxy or chlorine atom, improve the best interaction with active site of hMAO-B.
mBio, 6(4) (2015-08-27)
Considerable evidence exists that bacteria detect eukaryotic communication molecules and modify their virulence accordingly. In previous studies, it has been demonstrated that the increasingly antibiotic-resistant pathogen Pseudomonas aeruginosa can detect the human hormones brain natriuretic peptide (BNP) and C-type natriuretic
Organic letters, 17(1), 106-109 (2014-12-20)
The first catalytic enantioselective addition of thiols to ketimines derived from isatins has been developed. Excellent yields and enantioselectivities were observed for the reaction of various ketimines and thiols using a cinchona alkaloid sulfonamide catalyst. Both enantiomers of products could
Voprosy meditsinskoi khimii, 43(6), 515-521 (1998-03-21)
Isatin is an endogenous compound recently discovered in mammalian tissues and body fluids. It has a distinct distribution in rat brain, with a highest concentration, in the hippocampus, of 0.1 microgram/g. Its origin and metabolic pathways remain unclear. In vitro
Oncology reports, 32(5), 2111-2117 (2014-09-02)
Isatin is an endogenous indole in mammalian tissues and fluids that is expected to have antitumor effects in human breast cancer cells. Human breast cancer cells (MCF-7) were exposed to isatin at various concentrations (0, 50, 100, 200 µmol/l) for 48 h.
Bioorganic & medicinal chemistry letters, 19(9), 2509-2513 (2009-04-04)
Previous studies have shown that (E)-8-(3-chlorostyryl)caffeine (CSC) is a specific reversible inhibitor of human monoamine oxidase B (MAO-B) and does not bind to human MAO-A. Since the small molecule isatin is a natural reversible inhibitor of both MAO-B and MAO-A
Isatins as privileged molecules in design and synthesis of spiro-fused cyclic frameworks.
Chemical reviews, 112(11), 6104-6155 (2012-09-07)
Journal of inorganic biochemistry, 149, 49-58 (2015-05-30)
In this work, the influence of two new dinuclear copper(II) complexes in the viability of melanoma cells (B16F10 and TM1MNG3) was investigated, with the aim of verifying possible correlations between their cytotoxicity and their structure. One of the complexes had
Journal of medicinal chemistry, 56(11), 4509-4520 (2013-05-10)
The effector caspases-3 and -7 play a central role in programmed type I cell death (apoptosis). Molecular imaging using positron emission tomography (PET) by tracking the activity of executing caspases might allow the detection of the early onset as well
Journal of medicinal chemistry, 53(17), 6516-6520 (2010-08-19)
Novel 1-(4-arylthiazol-2-yl)-2-(3-methylcyclohexylidene)hydrazine derivatives have been investigated for their ability to inhibit selectively the activity of the human B isoform of monoamine oxidase. These compounds were obtained as racemates and (R)-enantiomers by a stereoconservative synthetic pattern in high yield and enantiomeric
Fitoterapia, 101, 51-56 (2015-01-01)
Human carbonyl reductase 1 (CBR1), a member of the short-chain dehydrogenase/reductase superfamily, reduces a variety of carbonyl compounds including therapeutic drugs. CBR1 is involved in the reduction of the anthracycline anticancer drugs to their less anticancer C-13 hydroxy metabolites, which
Journal of medicinal chemistry, 54(16), 5878-5889 (2011-07-05)
Cancer multidrug resistance (MDR) mediated by ATP-binding cassette (ABC) transporters presents a significant unresolved clinical challenge. One strategy to resolve MDR is to develop compounds that selectively kill cells overexpressing the efflux transporter P-glycoprotein (MDR1, P-gp, ABCB1). We have previously
Bioorganic & medicinal chemistry letters, 21(9), 2692-2696 (2011-01-11)
Inhibitors of human transglutaminase 2 (TG2) are anticipated to be useful in the therapy of a variety of diseases including celiac sprue as well as certain CNS disorders and cancers. A class of 3-acylidene-2-oxoindoles was identified as potent reversible inhibitors
Journal of medicinal chemistry, 50(8), 1876-1885 (2007-03-24)
Carboxylesterases (CE) are ubiquitous enzymes thought to be responsible for the metabolism and detoxification of xenobiotics. Numerous clinically used drugs including Demerol, lidocaine, capecitabine, and CPT-11 are hydrolyzed by these enzymes. Hence, the identification and application of selective CE inhibitors
European journal of medicinal chemistry, 58, 153-159 (2012-11-06)
The present manuscript describes the synthesis of uracil-isatin hybrids via azide-alkyne cycloadditions and their cytotoxic evaluation against three human cancer cell lines viz. HeLa (cervix), MCF-7 (breast) and DU145 (prostate) using MTT assay. The evaluation studies revealed the dependence of
Organic letters, 15(7), 1512-1515 (2013-03-13)
A highly stereo-, regio-, and chemoselective method has been devised for the synthesis of a wide range of spirooxindolyl oxazolidines via an intermolecular 1,3-dipolar cycloaddition of carbonyl ylides generated from dimethyl diazomalonate and aromatic aldehydes, with cyclic ketimines using 5
Journal of medicinal chemistry, 54(15), 5320-5334 (2011-07-06)
Tryptophan catabolism mediated by indoleamine 2,3-dioxygenase (IDO) is an important mechanism of peripheral immune tolerance contributing to tumoral immune resistance. IDO inhibition is thus an active area of research in drug development. Recently, our group has shown that tryptophan 2,3-dioxygenase
Vestnik Rossiiskoi akademii meditsinskikh nauk, (10)(10), 45-48 (1999-12-01)
Monoamine oxidase (MAO) catalyzes the biological degradation of the neurotransmitters monoamines. The altered substrate specificity of MAO may be of pathogenic importance in some cases and MAO inhibitors showed a therapeutical effect in the experimental setting. Analyzing the efficacy of
Organic letters, 13(18), 4782-4785 (2011-08-19)
A concise and efficient route for the synthesis of highly substituted imidazopyrroloquinoline derivatives by simply refluxing a reaction mixture of different types of isatins and heterocyclic ketene aminals (HKAs) by acetic acid was developed. This method is suitable for combinatorial
Bioorganic & medicinal chemistry, 21(7), 2025-2036 (2013-02-16)
Downstream caspases-3 and -7 are essential to execute the programmed type I cell death (apoptosis). In order to better understand their role, specific inhibitors of these enzymes are required, which after radiolabeling can be applied to non-invasively visualize and monitor
Journal of molecular modeling, 19(2), 727-735 (2012-10-12)
Isatin is an important compound from the biological aspect of view. It is an endogenous substance and moreover; various pharmacological activities have been reported for isatin and its derivatives. In-vitro cytotoxic effects of the prepared isatin Schiff bases toward HeLa
Pharmacological reports : PR, 65(2), 313-335 (2013-06-08)
Isatin, 1H-indole-2,3-dione, is a heterocyclic compound of significant importance in medicinal chemistry. It is a synthetically versatile molecule, a precursor for a large number of pharmacologically active compounds. Isatin and its derivatives have aroused great attention in recent years due
Palladium-catalyzed oxidative cycloaddition through C-H/N-H activation: access to benzazepines.
Angewandte Chemie (International ed. in English), 52(6), 1768-1772 (2013-01-03)
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