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Full-Text Articles in Life Sciences

The Potential Of Quinoline Derivatives For The Treatment Of Toxoplasma Gondii Infection., Sirinart Ananvoranich Oct 2014

The Potential Of Quinoline Derivatives For The Treatment Of Toxoplasma Gondii Infection., Sirinart Ananvoranich

Chemistry and Biochemistry Publications

Here we reported our investigation, as part of our drug repositioning effort, on anti-Toxoplasma properties of newly synthesized quinoline compounds. A collection of 4-aminoquinoline and 4-piperazinylquinoline analogs have recently been synthesized for use in cancer chemotherapy. Some analogs were able to outperform chloroquine, a quinoline derivative drug which is commonly used in the treatment of malaria and other parasitic infections. Herein 58 compounds containing one or two quinoline rings were examined for their effectiveness as potential anti-Toxoplasma compounds. Of these 58 compounds, 32 were efficient at inhibiting Toxoplasma growth (IC50μM). Five compounds with single and simple quinoline rings exhibited similar ...


Synthesis Of Tenuifolin Via Intramolecular Nicholas Reaction, Sinisa Djurdjevic, James R. Green Oct 2014

Synthesis Of Tenuifolin Via Intramolecular Nicholas Reaction, Sinisa Djurdjevic, James R. Green

Chemistry and Biochemistry Publications

The synthesis of the Cinnamomum homosesquiterpenoid tenuifolin has been accomplished by way of an intramolecular Nicholas reaction of the [Co2(CO)6] complex of an alkyne-substituted biaryl for construction of the seven-membered ring. The cyclization features the reaction of a nonactivated arene ring with the propargyldicobalt cation to give the dibenzocycloheptyne-Co2(CO)6.


Activated Cyclopropanes: A Remarkable Breadth Of Recent Chemistry, James R. Green, Victor Snieckus Oct 2014

Activated Cyclopropanes: A Remarkable Breadth Of Recent Chemistry, James R. Green, Victor Snieckus

Chemistry and Biochemistry Publications

The reactions of cyclopropanes activated by electron-withdrawing groups and electron-donating groups – donor–acceptor (DA) cyclopropanes – and with alkenyl or alkylidene substituents has been an area of recent intense research activity. This Cluster contains contributions from many of the leading research groups in this area, and provides a concise introduction to the rich ring-opening, ring-expansion, dimerization, and cycloaddition chemistry of these compounds.


A Multi-Scale Computational Study On The Mechanism Of Streptococcus Pneumoniae Nicotinamidase (Spnic), Bogdan F. Ion, Erum Kazim, James Gauld Sep 2014

A Multi-Scale Computational Study On The Mechanism Of Streptococcus Pneumoniae Nicotinamidase (Spnic), Bogdan F. Ion, Erum Kazim, James Gauld

Chemistry and Biochemistry Publications

Nicotinamidase (Nic) is a key zinc-dependent enzyme in NAD metabolism that catalyzes the hydrolysis of nicotinamide to give nicotinic acid. A multi-scale computational approach has been used to investigate the catalytic mechanism, substrate binding and roles of active site residues of Nic from Streptococcus pneumoniae (SpNic). In particular, density functional theory (DFT), molecular dynamics (MD) and ONIOM quantum mechanics/molecular mechanics (QM/MM) methods have been employed. The overall mechanism occurs in two stages: (i) formation of a thioester enzyme-intermediate (IC2) and (ii) hydrolysis of the thioester bond to give the products. The polar protein environment has a significant effect ...


Novel Analogue Of Colchicine Induces Selective Pro-Death Autophagy And Necrosis In Human Cancer Cells, Kristen Elizabeth Larocque, Pamela Ovadje, Sinisa Djurdjevic, Mariam Mehdi, James R. Green, Siyaram Pandey Jan 2014

Novel Analogue Of Colchicine Induces Selective Pro-Death Autophagy And Necrosis In Human Cancer Cells, Kristen Elizabeth Larocque, Pamela Ovadje, Sinisa Djurdjevic, Mariam Mehdi, James R. Green, Siyaram Pandey

Chemistry and Biochemistry Publications

Colchicine, a natural product of Colchicum autumnae currently used for gout treatment, is a tubulin targeting compound which inhibits microtubule formation by targeting fast dividing cells. This tubulin-targeting property has lead researchers to investigate the potential of colchicine and analogs as possible cancer therapies. One major study conducted on an analogue of allocolchicine, ZD 6126, was halted in phase 2 clinical trials due to severe cardio-toxicity associated with treatment. This study involves the development and testing of novel allocolchicine analogues that hold non-toxic anti-cancer properties. Currently we have synthesized and evaluated the anti-cancer activities of two analogues; N-acetyl-O-methylcolchinol (NSC 51046 ...