Search Results - "Heise, Niels V"

Synthesis of Rhodamine-Conjugated Lupane Type Triterpenes of Enhanced Cytotoxicity by Denner, Toni C, Heise, Niels V, Hoenke, Sophie, Csuk, René

“…Various conjugates with rhodamines were prepared by starting with betulinic acid ( ) and platanic acid ( ). The molecules homopiperazine and piperazine, which…”
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F16 Hybrids Derived from Steviol or Isosteviol Are Accumulated in the Mitochondria of Tumor Cells and Overcome Drug Resistance by Heise, Niels V, Heisig, Julia, Meier, Kristof, Csuk, René, Mueller, Thomas

“…Steviol and isosteviol were prepared from the commercially available sweetener stevioside and converted into lipophilic F16 hybrids. Their cytotoxicity was…”
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Synthesis and In Silico Docking Study towards M-Pro of Novel Heterocyclic Compounds Derived from Pyrazolopyrimidinone as Putative SARS-CoV-2 Inhibitors by Horchani, Mabrouk, Heise, Niels V, Csuk, René, Ben Jannet, Hichem, Harrath, Abdel Halim, Romdhane, Anis

“…In addition to vaccines, antiviral drugs are essential in order to suppress COVID-19. Although some inhibitor candidates have been determined to target the…”
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Rhodamine 101 Conjugates of Triterpenoic Amides Are of Comparable Cytotoxicity as Their Rhodamine B Analogs by Heise, Niels V, Major, Daniel, Hoenke, Sophie, Kozubek, Marie, Serbian, Immo, Csuk, René

“…Pentacyclic triterpenoic acids (betulinic, oleanolic, ursolic, and platanic acid) were selected and subjected to acetylation followed by the formation of…”
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Synthesis and Enzymatic Evaluation of a Small Library of Substituted Phenylsulfonamido-Alkyl Sulfamates towards Carbonic Anhydrase II by Denner, Toni C, Heise, Niels V, Al-Harrasi, Ahmed, Csuk, René

“…A small library of 79 substituted phenylsulfonamidoalkyl sulfamates, - , was synthesized starting from arylsulfonyl chlorides and amino alcohols with different…”
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The Finally Rewarding Search for A Cytotoxic Isosteviol Derivative by Heisig, Julia, Heise, Niels V, Hoenke, Sophie, Ströhl, Dieter, Csuk, René

“…Acid hydrolysis of stevioside resulted in a 63% yield of isosteviol ( ), which served as a starting material for the preparation of numerous amides. These…”
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Developing an Amide-Spacered Triterpenoid Rhodamine Hybrid of Nano-Molar Cytotoxicity Combined with Excellent Tumor Cell/Non-Tumor Cell Selectivity by Heise, Niels V, Denner, Toni C, Becker, Selina, Hoenke, Sophie, Csuk, René

“…Asiatic acid, a pentacyclic triterpene, was converted into a series of piperazinyl, homopiperazinyl, and 1,5-diazocinyl spacered rhodamine conjugates,…”
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Stereochemistry matters: Inhibition of carbonic anhydrase II by amino acid derived sulfamates depends on their absolute configuration by Denner, Toni C., Klett, Elsa L., Heise, Niels V., Csuk, René

“…Aminoalcohols were converted into the corresponding enantiomeric phenylsulfonamide sulfamates. These compounds proved to be inhibitors of carbonic anhydrase…”
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Synthesis and In Silico Docking of New Pyrazolo[4,3-e]pyrido[1,2-a]pyrimidine-based Cytotoxic Agents by Horchani, Mabrouk, Heise, Niels V., Hoenke, Sophie, Csuk, René, Harrath, Abdel Halim, Ben Jannet, Hichem, Romdhane, Anis

“…To explore a new set of anticancer agents, a novel series of pyrazolo[4,3-e]pyrido[1,2-a]pyrimidine derivativeshave been designed and synthesized…”
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Combination of Betulinic Acid Fragments and Carbonic Anhydrase Inhibitors-A New Drug Targeting Approach by Bache, Matthias, Heise, Niels V, Thiel, Andreas, Funtan, Anne, Seifert, Franziska, Petrenko, Marina, Güttler, Antje, Brandt, Sarah, Mueller, Thomas, Vordermark, Dirk, Thondorf, Iris, Csuk, René, Paschke, Reinhard

“…Human carbonic anhydrase IX (hCA IX) is a zinc(II)-dependent metalloenzyme that plays a critical role in the conversion of carbon dioxide and water to protons…”
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Dehydroabietylamine-substituted trifluorobenzene sulfonamide rhodamine B hybrids as anticancer agents overcoming drug resistance by Heise, Niels V., Meyer, Sven J., Csuk, René, Mueller, Thomas

“…Attachment of a conjugate assembled from a novel fluorinated carbonic anhydrase inhibitor and rhodamine B onto dehydroabietylamine (DHA) or cyclododecylamine…”
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Betulinic acid derived amides are highly cytotoxic, apoptotic and selective by Hoenke, Sophie, Heise, Niels V., Kahnt, Michael, Deigner, Hans-Peter, Csuk, René

“…Betulinic and platanic acid derived amides were prepared and screened for their cytotoxic activity. All of the compounds were shown to be cytotoxic for a panel…”
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Asiatic acid as a leading structure for derivatives combining sub-nanomolar cytotoxicity, high selectivity, and the ability to overcome drug resistance in human preclinical tumor models by Kraft, Oliver, Hartmann, Anne-Kathrin, Brandt, Sarah, Hoenke, Sophie, Heise, Niels V., Csuk, René, Mueller, Thomas

“…Amides and rhodamine B conjugates of different pentacyclic triterpene acids have been shown outstanding cytotoxicity for human tumor cells. Starting from…”
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Inhibitory properties of quinopimaric acid derivatives towards cholinesterases by Tretyakova, Elena, Heise, Niels V., Csuk, René, Kazakova, Oxana

“…A series of new diterpene quinopimaric acid derivatives modified at the hydroxyl group with different pharmacophore fragments has been synthesised and their…”
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An asiatic acid derived trisulfamate acts as a nanomolar inhibitor of human carbonic anhydrase VA by Denner, Toni C., Heise, Niels V., Serbian, Immo, Angeli, Andrea, Supuran, Claudiu T., Csuk, René

“…[Display omitted] •Triterpenoic acids benzylamides were synthesized and sulfamoylated.•These compounds were tested as inhibitors of carbonic anhydrases (CA) I,…”
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Diethoxyphosphoryloxy‐oleanolic acid is a nanomolar‐inhibitor of butyrylcholinesterase by Petrova, Anastasiya V., Poptsov, Alexandr I., Heise, Niels V., Csuk, René, Kazakova, Oxana B.

“…A series of new betulin, lupeol, erythrodiol, and oleanolic acid phosphoryloxy‐ and furoyloxy‐derivatives has been synthesized and their structure was…”
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Acetylcholinesterase Inhibitory Activity of Modified Lupane, Oleanane, and Ursane A‐seco‐Triterpenoids by Petrova, Anastasiya V., Kazakova, Oxana B., Nazarov, Ivan S., Csuk, René, Heise, Niels V.

“…A series of new lupane, ursane, and oleanane type triterpenic A‐seco‐derivatives containing bromo‐, azido‐, alkyne‐, 1H‐tetrazol‐5‐yl‐, 5‐methyloxazol‐2‐yl‐,…”
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(Iso)quinoline amides derived from corosolic acid exhibit high cytotoxicity, and the potential for overcoming drug resistance in human cancer cells by Heise, Niels V., Csuk, René, Mueller, Thomas

“…Previous research on acetylated pentacyclic triterpenes had demonstrated the excellent cytotoxic action and, in certain situations, very surprising selectivity…”
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Revisiting capsaicin and nonivamide: Their analogs exert strong inhibitory activity against cholinesterases by Heise, Niels V., Quast, Jeremy, Csuk, René

“…The scientific community has long been interested in capsaicin, and the extensive hunt for AChE and BChE enzyme inhibitors is still ongoing. In this…”
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Arylsulfonamido-alkyl-sulfamates act as inhibitors of bovine carbonic anhydrase II by Denner, Toni C., Heise, Niels V., Csuk, René

“…A small library of arylsulfonamido-alkyl sulfamates was prepared by a two-step synthesis from readily available starting materials. The compounds were tested…”
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