Fragment‐Based Design, Synthesis, and Biological Evaluation of 1‐Substituted‐indole‐2‐carboxylic Acids as Selective Mcl‐1 Inhibitors
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DOI: 10.1002/ardp.201600251
Abstract: Based on a known selective Mcl‐1 inhibitor, 6‐chloro‐3‐(3‐(4‐chloro‐3,5‐dimethylphenoxy)propyl)‐1H‐indole‐2‐carboxylic acid, we applied a fragment‐based approach to obtain new molecules that extended into the p1 pocket of the BH3 groove and then exhibited binding selectivity for the… read more here.
Keywords: mcl; indole carboxylic; selective mcl; fragment based ... See more keywords
[Carboxyl‐11C]Labelling of Four High‐Affinity cPLA2α Inhibitors and Their Evaluation as Radioligands in Mice by Positron Emission Tomography
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DOI: 10.1002/cmdc.201700697
Abstract: Cytosolic phospholipase A2α (cPLA2α) may play a critical role in neuropsychiatric and neurodegenerative disorders associated with oxidative stress and neuroinflammation. An effective PET radioligand for imaging cPLA2α in living brain might prove useful for biomedical… read more here.
Keywords: four high; indole carboxylic; cpla2; carboxylic acid ... See more keywords
Engineering of a chromogenic enzyme screening system based on an auxiliary indole‐3‐carboxylic acid monooxygenase
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DOI: 10.1002/mbo3.795
Abstract: Here, we present a proof‐of‐principle for a new high‐throughput functional screening of metagenomic libraries for the selection of enzymes with different activities, predetermined by the substrate being used. By this approach, a total of 21… read more here.
Keywords: screening system; indole carboxylic; carboxylic acid; system based ... See more keywords
METHODS FOR THE SYNTHESIS OF INDOLE-3-CARBOXYLIC ACID ESTERS
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DOI: 10.1007/4728
Abstract: In this microreview, recent advances in the development of methods for indole cyclization, leading to indole-3-carboxylic acid derivatives, are highlighted. Selected works published since 2013 are covered. Authors: Valeriya A. Litvinova, Alexander S. Tikhomirov read more here.
Keywords: methods synthesis; indole carboxylic; acid esters; carboxylic acid ... See more keywords
Heterocyclic Analogs of 5,12-Naphthacenequinone 14*. Synthesis of naphtho[2,3-f]indole-3-carboxylic Acid Derivatives
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DOI: 10.1007/s10593-017-2173-y
Abstract: 3-carboxylate by using vicarious substitution of hydrogen, followed by intramolecular reductive heterocyclization. Some chemical properties of the target compound were characterized. As observed for the first time in the series of linear hetaryl-fused anthraquinones, the… read more here.
Keywords: naphtho indole; naphthacenequinone synthesis; heterocyclic analogs; indole carboxylic ... See more keywords
Methods for the synthesis of indole-3-carboxylic acid esters (microreview)
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DOI: 10.1007/s10593-018-2370-3
Abstract: In this microreview, recent advances in the development of methods for indole cyclization, leading to indole-3-carboxylic acid derivatives, are highlighted. Selected works published since 2013 are covered. read more here.
Keywords: methods synthesis; indole carboxylic; acid esters; carboxylic acid ... See more keywords
Structure-activity relationship studies on 1-(2-oxopropyl)indole-5-carboxylic acids acting as inhibitors of cytosolic phospholipase A2α: Effect of substituents at the indole 3-position on activity, solubility, and metabolic stability.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2016.10.039
Abstract: Cytosolic phospholipase A2α (cPLA2α) is a key enzyme in the biosynthesis of pro-inflammatory lipid mediators and therefore represents an attractive target for the development of new anti-inflammatory drugs. Recently, we have found that 1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid… read more here.
Keywords: cytosolic phospholipase; indole carboxylic; oxopropyl indole; effect ... See more keywords
A concise and regioselective synthesis of 6-bromo-5-methoxy-1H-indole-3-carboxylic acid and its derivatives: Strategic development toward core moiety of Herdmanine D
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DOI: 10.1080/00397911.2020.1718162
Abstract: Abstract A concise, regioselective and highly efficient strategy for the construction of 6-bromo-5-methoxy-1H-indole-3-carboxylic acid has been developed through trifluoroacetylated indole driven hydrolysis. The developed protocol has the advantage of selectively directing bromine substituent on one… read more here.
Keywords: indole carboxylic; carboxylic acid; methoxy indole; bromo methoxy ... See more keywords