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Articles 1 - 14 of 14
Full-Text Articles in Physical Sciences and Mathematics
Anti-Cancer Activity Of An Acid-Labile N-Alkylisatin Conjugate Targeting The Transferrin Receptor, Vineesh Indira Chandran, Lidia Matesic, Julie Locke, Danielle Skropeta, Marie Ranson, Kara Vine
Anti-Cancer Activity Of An Acid-Labile N-Alkylisatin Conjugate Targeting The Transferrin Receptor, Vineesh Indira Chandran, Lidia Matesic, Julie Locke, Danielle Skropeta, Marie Ranson, Kara Vine
Danielle Skropeta
We have previously reported a series of pH-sensitive imine-linked N-alkylisatin prodrugs that are stable at pH 7.4, but readily cleaved at pH 4.5. Herein, one of the most potent prodrugs, 5,7-dibromo-N-(pmethoxybenzyl) isatin (NAI), was functionalized with a para-phenylpropionic acid linker, and the resulting NAI–imine prodrug conjugated to transferrin (Tf) to form a NAI–imine–Tf conjugate. Cytotoxicity assays revealed the conjugate was equipotent to the free drug against MCF-7 breast cancer cells, with clear selectivity patterns based on TfR levels. These results suggest that this novel isatin-based cytotoxin conjugated to a tumor targeting protein via an acid-labile linker warrants further preclinical testing.
The Effect Of Individual N-Glycans On Enzyme Activity, Danielle Skropeta
The Effect Of Individual N-Glycans On Enzyme Activity, Danielle Skropeta
Danielle Skropeta
No abstract provided.
Domino Pericyclic Reactions Of Acyclic Conjugated (E,Z,E,E)-Tetraenes, Danielle Skropeta, Rodney Rickards
Domino Pericyclic Reactions Of Acyclic Conjugated (E,Z,E,E)-Tetraenes, Danielle Skropeta, Rodney Rickards
Danielle Skropeta
No abstract provided.
N-Phenethyl And N-Naphthylmethyl Isatins And Analogues As In Vitro Cytotoxic Agents, John Bremner, Stephen Pyne, Marie Ranson, Danielle Skropeta, Julie Locke, Lidia Matesic, Kara Perrow
N-Phenethyl And N-Naphthylmethyl Isatins And Analogues As In Vitro Cytotoxic Agents, John Bremner, Stephen Pyne, Marie Ranson, Danielle Skropeta, Julie Locke, Lidia Matesic, Kara Perrow
Danielle Skropeta
Arange of N-phenethyl,N-phenacyl, and N-(1- and 2-naphthylmethyl) derivatives of 5,7-dibromoisatin 2 were prepared byN-alkylation reactions. Their activity against human monocyte-like histiocytic lymphoma (U937), leukemia (Jurkat), and breast carcinoma (MDA-MB-231) cell lines was assessed. The results allowed further development of structureactivity relationships. The compound 5,7-dibromo-N-(1-naphthylmethyl)-1H-indole-2,3-dione 5a was the most potent against U937 cells with an IC50 value of 0.19 microM.
Complete Assignment Of The 1h And 13c Nmr Spectra Of Antimicrobial 4-Arylamino- 3-Nitrocoumarin Derivatives, Vidoslav Dekic, Niko Radulovic, Rastko Vukicevic, Biljana Dekic, Danielle Skropeta, Radosav Palic
Complete Assignment Of The 1h And 13c Nmr Spectra Of Antimicrobial 4-Arylamino- 3-Nitrocoumarin Derivatives, Vidoslav Dekic, Niko Radulovic, Rastko Vukicevic, Biljana Dekic, Danielle Skropeta, Radosav Palic
Danielle Skropeta
No abstract provided.
Synthesis And Hydrolytic Evaluation Of Acid-Labile Imine-Linked Cytoxic Isatin Model Systems, Lidia Matesic, Julie Locke, Kara Perrow, Marie Ranson, John Bremner, Danielle Skropeta
Synthesis And Hydrolytic Evaluation Of Acid-Labile Imine-Linked Cytoxic Isatin Model Systems, Lidia Matesic, Julie Locke, Kara Perrow, Marie Ranson, John Bremner, Danielle Skropeta
Danielle Skropeta
In this study a series of isatin-based, pH-sensitive aryl imine derivatives with differing aromatic substituents and substitution patterns were synthesised and their acid-catalysed hydrolysis evaluated. These derivatives were functionalised at the C3 carbonyl group of a potent N-substituted isatin cytotoxin and were stable at physiological pH but readily cleaved at pH 4.5. Observed rates of hydrolysis for the embedded imine-acid moiety were in the order para-phenylpropionic acid>phenylacetic acid (para>meta)>benzoic acid (meta>para). The ability to fine-tune hydrolysis rates in this way has potential implications for optimising imine linked, tumour targeting cytotoxin-protein conjugates
N-Glycolisation Regulates Endothelial Lipase-Mediated Phospholipid Hydrolysis In Apoe- And Apoa-I-Containing High Density Lipoproteins, Danielle Skropeta, Daniel Rader, Weijun Jin, Monica Mcmahon, Kate Shearston, Philip Barter, Kristine Mcgrath, Kerry-Anne Rye, Chatri Settasatian, Daniela Caiazza
N-Glycolisation Regulates Endothelial Lipase-Mediated Phospholipid Hydrolysis In Apoe- And Apoa-I-Containing High Density Lipoproteins, Danielle Skropeta, Daniel Rader, Weijun Jin, Monica Mcmahon, Kate Shearston, Philip Barter, Kristine Mcgrath, Kerry-Anne Rye, Chatri Settasatian, Daniela Caiazza
Danielle Skropeta
No abstract provided.
Cytotoxic And Anticancer Activities Of Isatin And Its Derivatives: A Comprehensive Review From 2000-2008, Marie Ranson, Danielle Skropeta, Julie Locke, Lidia Matesic, Kara Perrow
Cytotoxic And Anticancer Activities Of Isatin And Its Derivatives: A Comprehensive Review From 2000-2008, Marie Ranson, Danielle Skropeta, Julie Locke, Lidia Matesic, Kara Perrow
Danielle Skropeta
No abstract provided.
Chemotaxonomy Of The Peppergrass Lepidium Coronopus (L.) Al-Shehbaz (Syn. Coronopus Squamatus) Based On Its Volatile Glucosinolate Autolysis Products, Niko Radulovic, Bojan Zlatkovic, Danielle Skropeta, Radosav Palic´
Chemotaxonomy Of The Peppergrass Lepidium Coronopus (L.) Al-Shehbaz (Syn. Coronopus Squamatus) Based On Its Volatile Glucosinolate Autolysis Products, Niko Radulovic, Bojan Zlatkovic, Danielle Skropeta, Radosav Palic´
Danielle Skropeta
The genus Lepidium comprises approximately 175 different plant species commonly referred to as peppergrasses or pepperworts ( Al-Shehbaz, 1997 and Mummenhoff et al., 2001), which occur worldwide apart from the polar regions where they are considered rare in the Arctic and are absent from Antarctica. Lepidium is a comparatively large genus belonging to the mustard family Brassicaceae. Lepidium coronopus (L.) Al-Shehbaz, a representative of the genus, is a herbaceous annual to biennial plant that belongs to the tribe Lepidieae and has previously been described by the following synonymous species: Coronopus squamatus (Forsskal) Ascherson; C. squamatus subsp. conradi (Muschler) Maire; C. …
Apolipoprotein J And Leptin Levels In Patients With Coronary Heart Disease, Mark Wilson, Dimitri Mikhailidis, Maria Poulakou, Christos Tsigris, Despina Perrea, Kosmas Paraskevas, Dimitrios Iliopoulos
Apolipoprotein J And Leptin Levels In Patients With Coronary Heart Disease, Mark Wilson, Dimitri Mikhailidis, Maria Poulakou, Christos Tsigris, Despina Perrea, Kosmas Paraskevas, Dimitrios Iliopoulos
Mark R Wilson
No abstract provided.
Ozone-Induced Dissociation On A Modified Tandem Linear Ion-Trap: Observations Of Different Reactivity For Isomeric Lipids, Berwyck Poad, Huong Pham, Michael Thomas, Jessica Hughes, J Campbell, Todd Mitchell, Stephen Blanksby
Ozone-Induced Dissociation On A Modified Tandem Linear Ion-Trap: Observations Of Different Reactivity For Isomeric Lipids, Berwyck Poad, Huong Pham, Michael Thomas, Jessica Hughes, J Campbell, Todd Mitchell, Stephen Blanksby
Berwyck L. J. Poad
Ozone-induced dissociation (OzID) exploits the gas-phase reaction between mass-selected lipid ions and ozone vapor to determine the position(s) of unsaturation. In this contribution, we describe the modification of a tandem linear ion-trap mass spectrometer specifically for OzID analyses wherein ozone vapor is supplied to the collision cell. This instrumental configuration provides spatial separation between mass-selection, the ozonolysis reaction, and mass-analysis steps in the OzID process and thus delivers significant enhancements in speed and sensitivity (ca. 30-fold). These improvements allow spectra revealing the double-bond position(s) within unsaturated lipids to be acquired within 1 s: significantly enhancing the utility of OzID in …
Synthesis Of Functionalised 2-Aryl-5-Nitro-1h-Indoles And Their Activity As Bacterial Nora Efflux Pump Inhibitors, John Bremner, Siritron Samosorn, Anthony Ball, Kim Lewis
Synthesis Of Functionalised 2-Aryl-5-Nitro-1h-Indoles And Their Activity As Bacterial Nora Efflux Pump Inhibitors, John Bremner, Siritron Samosorn, Anthony Ball, Kim Lewis
Kim Lewis
No abstract provided.
Conjugating Berberine To A Multidrug Resistance Pump Inhibitor Creates An Effective Antimicrobial, John Bremner, Siritron Samosorn, Anthony Ball, Gabriele Casadei, Terence Moy, Frederik Ausubel, Kim Lewis
Conjugating Berberine To A Multidrug Resistance Pump Inhibitor Creates An Effective Antimicrobial, John Bremner, Siritron Samosorn, Anthony Ball, Gabriele Casadei, Terence Moy, Frederik Ausubel, Kim Lewis
Kim Lewis
No abstract provided.
Structure-Activity Relationships Of 2-Aryl-1h-Indole Inhibitors Of The Nora Efflux Pump In Staphylococcus Aureus, John Bremner, Michael Kelso, Joseph Ambrus, Kim Lewis, Anthony Ball, Gabriele Casadei
Structure-Activity Relationships Of 2-Aryl-1h-Indole Inhibitors Of The Nora Efflux Pump In Staphylococcus Aureus, John Bremner, Michael Kelso, Joseph Ambrus, Kim Lewis, Anthony Ball, Gabriele Casadei
Kim Lewis
The synthesis of 22 2-aryl-1H-indoles, including 12 new compounds, has been achieved via Pd- or Rh-mediated methodologies, or selective electrophilic substitution. All three methods were based on elaborations from simple indole precursors. SAR studies on these indoles and 2-phenyl-1H-indole in Staphylococcus aureus as NorA efflux pump inhibitors indicated 5-nitro-2-(3-methoxycarbonyl)phenyl-1H-indole was a slightly more potent inhibitor than the lead INF55. A promising new antibacterial lead compound against S. aureus (2-phenyl-1H-indol-5-yl)-methanol, was also found.