- A Screening Platform to Identify and Tailor Biocompatible Small-Molecule Catalysts
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Interfacing biocompatible, small-molecule catalysis with cellular metabolism promises a straightforward introduction of new function into organisms without the need for genetic manipulation. However, identifying and optimizing synthetic catalysts that per
- Ivanov, Ilya,Mayer, Clemens,Rubini, Rudy
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supporting information
p. 16017 - 16021
(2019/11/28)
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- Synthesis and antiplasmodial evaluation of novel (4-aminobutyloxy) quinolines
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A variety of 5-, 6- and 8-(4-aminobutyloxy)quinolines as novel oxygen analogues of known 4- and 8-(4-aminobutylamino)quinoline antimalarial drugs was generated from hydroxyquinolines through a three-step approach with a rhodium-catalyzed hydroformylation
- Vandekerckhove, Stéphanie,Müller, Christian,Vogt, Dieter,Lategan, Carmen,Smith, Peter J.,Chibale, Kelly,De Kimpe, Norbert,D'Hooghe, Matthias
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supporting information
p. 318 - 322
(2013/02/23)
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- Evaluation of (4-aminobutyloxy)quinolines as a novel class of antifungal agents
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Antifungal assessment of eighteen 5-, 6- and 8-(4-aminobutyloxy)quinolines revealed a significant susceptibility of the tested fungi and yeast strains (Candida albicans, Rhodotorula bogoriensis, Aspergillus flavus and Fusarium solani) toward different hal
- Vandekerckhove, Stéphanie,Tran, Hai Giang,Desmet, Tom,D'Hooghe, Matthias
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p. 4641 - 4643
(2013/08/23)
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- Substituted oxines inhibit endothelial cell proliferation and angiogenesis
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Two substituted oxines, nitroxoline (5) and 5-chloroquinolin-8-yl phenylcarbamate (22), were identified as hits in a high-throughput screen aimed at finding new anti-angiogenic agents. In a previous study, we have elucidated the molecular mechanism of antiproliferative activity of nitroxoline in endothelial cells, which comprises of a dual inhibition of type 2 human methionine aminopeptidase (MetAP2) and sirtuin 1 (SIRT1). Structure-activity relationship study (SAR) of nitroxoline offered many surprises where minor modifications yielded oxine derivatives with increased potency against human umbilical vein endothelial cells (HUVEC), but with entirely different as yet unknown mechanisms. For example, 5-nitrosoquinolin-8-ol (33) inhibited HUVEC growth with sub-micromolar IC50, but did not affect MetAP2 or MetAP1, and it only showed weak inhibition against SIRT1. Other sub-micromolar inhibitors were derivatives of 5-aminoquinolin-8-ol (34) and 8-sulfonamidoquinoline (32). A sulfamate derivative of nitroxoline (48) was found to be more potent than nitroxoline with the retention of activities against MetAP2 and SIRT1. The bioactivity of the second hit, micromolar HUVEC and MetAP2 inhibitor carbamate 22 was improved further with an SAR study culminating in carbamate 24 which is a nanomolar inhibitor of HUVEC and MetAP2. The Royal Society of Chemistry 2012.
- Bhat, Shridhar,Shim, Joong Sup,Zhang, Feiran,Chong, Curtis Robert,Liu, Jun O.
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supporting information; experimental part
p. 2979 - 2992
(2012/05/07)
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- Palladium-catalyzed 8-exo trig intramolecular heck reaction under microwave irradiation in the presence of basic alumina
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The Heck cross-coupling reaction has been employed for efficient conversion of quinolines to benzoxocinoquinoline through a microwave-assisted palladium-catalyzed intramolecular cyclization in the presence of basic alumina.
- Saha, Pritam,Mondal, Shyamal,Hazra, Abhijit,Naskar, Subhendu,Maity, Arindam,Sahu, Krishnendu B.,Paira, Rupankar,Das, Saktipada,Banerjee, Sukdeb,Mondal, Nirup B.
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p. 3166 - 3176
(2012/11/07)
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- QUINOLINE COMPOUNDS AS INHIBITORS OF ANGIOGENESIS, HUMAN METHIONINE AMINOPEPTIDASE, AND SIRT1, AND METHODS OF TREATING DISORDERS
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Described herein are methods of inhibiting methionine aminopeptidase or SirT1, inhibiting angiogenesis, and treating disorders (or symptoms thereof) associated with methionine aminopeptidase, SirT1 and/or angiogenesis, wherein a compound of the invention
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Page/Page column 64
(2010/04/28)
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- 8-HYDROXYQUINOLINE COMPOUNDS AND METHODS THEREOF
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The present invention relates to 8-Hydroxyquinoline Compounds; compositions comprising an 8-Hydroxyquinoline Compound; and methods for treating or preventing a metalloproteinase-related disorder, such as, an arthritic disorder, osteoarthritis, malignant neoplasm, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, atherosclerosis, age-related macular degeneration, myocardial infarction, a corneal ulceration, an ocular surface disease, hepatitis, an aortic aneurysm, tendonitis, a central nervous system disorder, abnormal wound healing, angiogenesis, restenosis, cirrhosis, multiple sclerosis, glomerulonephritis, graft versus host disease, diabetes, an inflammatory bowel disease, shock, invertebral disc degeneration, stroke, osteopenia or a periodontal disease or comprising administering an effective dose of an 8-Hydroxyquinoline Compound to a mammal in need thereof.
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Page/Page column 83-84
(2008/06/13)
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- Quinoline derivatives and compositions thereof for the protection of cultivated plants
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There are used for the protection of cultivated plants against the harmful effects of agricultural chemicals quinoline derivatives of the formula STR1 wherein R1, R2 and R3 independently of one another are each hydrogen, halogen, nitro, cyano, alkyl, alkoxy or acyl, R4, R5 and R6 independently of one another are each hydrogen, halogen or alkyl, X is an aliphatic, saturated or unsaturated, straight-chain or branched-chain hydrocarbon radical which has 1 to 12 carbon atoms and which can be interrupted by one or more hetero atoms or can be substituted by halogen, and Y is hydrogen, halogen, hydroxyl, alkoxy, alkenyloxy, alkynyloxy, a substituted amino group, an ammonio group, a cycloaliphatic radical, a heterocyclic radical which is substituted or substituted by alkyl having 1 to 4 carbon atoms, or is phenyl which is unsubstituted or substituted, or is aryloxy which is unsubstituted or substituted, or is benzyloxy which is unsubstituted or substituted, or is acyloxy, with the inclusion of the acid addition salts and metal complexes thereof; or there are used compositions which contain such derivatives. Also described are novel quinoline derivatives and the production thereof.
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