Amelia Vom

Structure-Guided Development of Potent Benzoylurea Inhibitors of BCL-X-L and BCL-2

Michael J Roy, Amelia Vom, Toru Okamoto, Brian J Smith, Richard W Birkinshaw, Hong Yang, Houda Abdo, Christine A White, David Segal, David CS Huang, Jonathan B Baell, Peter M Colman, Peter E Czabotar, Guillaume Lessene

Journal article  |  2021  |  JOURNAL OF MEDICINAL CHEMISTRY

The BCL-2 family of proteins (including the prosurvival proteins BCL-2, BCL-XL, and MCL-1) is an important target for the developm..

Cell death and the mitochondria: therapeutic targeting of the BCL-2 family-driven pathway

MJ Roy, A Vom, PE Czabotar, G Lessene

Journal article  |  2014  |  BRITISH JOURNAL OF PHARMACOLOGY

The principal biological role of mitochondria is to supply energy to cells; although intriguingly, evolution has bestowed another ..

De-Novo Designed Library of Benzoylureas as Inhibitors of BCL-X-L: Synthesis, Structural and Biochemical Characterization

Ryan M Brady, Amelia Vom, Michael J Roy, Nathan Toovey, Brian J Smith, Rebecca M Moss, Effie Hatzis, David CS Huang, John P Parisot, Hong Yang, Ian P Street, Peter M Colman, Peter E Czabotar, Jonathan B Baell, Guillaume Lessene

Journal article  |  2014  |  JOURNAL OF MEDICINAL CHEMISTRY

The prosurvival BCL-2 proteins are attractive yet challenging targets for medicinal chemists. Their involvement in the initiation ..

Detection and Prevention of Aggregation-based False Positives in STD-NMR-based Fragment Screening

Amelia Vom, Stephen Headey, Geqing Wang, Ben Capuano, Elizabeth Yuriev, Martin J Scanlon, Jamie S Simpson

Journal article  |  2013  |  AUSTRALIAN JOURNAL OF CHEMISTRY

Aggregation of small organic compounds is a problem encountered in a variety of assay screening formats where it often results in ..

Remarkable in vitro bactericidal activity of bismuth(III) sulfonates against Helicobacter pylori

Philip C Andrews, Madleen Busse, Glen B Deacon, Richard L Ferrero, Peter C Junk, Jonathan G MacLellan, Amelia Vom

Journal article  |  2012  |  DALTON TRANSACTIONS

Four new tris-substituted bismuth(III) sulfonates of general formula [Bi(O(3)SR)(3)] (R = phenyl 1, p-tolyl 2, 2,4,6-mesityl 3 and..

New hybrids of clozapine and haloperidol and their isosteric analogues: synthesis, X-ray crystallography, conformational analysis and preliminary pharmacological evaluation

Ben Capuano, Ian T Crosby, Craig M Forsyth, Fiona M McRobb, Vladimir V Moudretski, David A Taylor, Amelia Vom, Elizabeth Yuriev

Journal article  |  2010  |  STRUCTURAL CHEMISTRY

Schizophrenia is a debilitating mental disorder which affects approximately 1% of the world's population. Clozapine is an atypical..

JL13 has clozapine-like actions on thermoregulatory cutaneous blood flow in rats: Involvement of serotonin 5-HT1A and 5-HT2A receptor mechanisms

B Capuano, IT Crosby, FM McRobb, DA Taylor, A Vom, WW Blessing

Journal article  |  2010  |  PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY

Clozapine is an effective atypical antipsychotic agent, with serious side effects. JL13 [5-(4-methylpiperazin-1-yl)-8-chloropyrido..

The Synthesis and Preliminary Pharmacological Evaluation of a Series of Substituted 4 '-Phenoxypropyl Analogues of the Atypical Antipsychotic Clozapine

Ben Capuano, Ian T Crosby, Fiona M McRobb, Anna Podloucka, David A Taylor, Amelia Vom, Elizabeth Yuriev

Journal article  |  2010  |  AUSTRALIAN JOURNAL OF CHEMISTRY

Herein we report the synthesis, characterization, and preliminary pharmacological activity of a new series of substituted 4′-pheno..

8-chloro-5-(4-phenethylpiperazin-1-yl)-pyrido[2,3-b][1,5]benzoxazepine

Ben Capuano, Ian T Crosby, Craig M Forsyth, Edward J Lloyd, Amelia Vom, Elizabeth Yuriev

Journal article  |  2008  |  ACTA CRYSTALLOGRAPHICA SECTION E-CRYSTALLOGRAPHIC COMMUNICATIONS

As part of an anti-psychotic drug discovery program, we report the crystal structure of the title compound, C(24)H(23)ClN(4)O. The..

Backbone assignments of the 34 kDa ketopantoate reductase from E. coli

Stephen J Headey, Amelia Vom, Jamie S Simpson, Martin J Scanlon

Journal article  |  2008  |  BIOMOLECULAR NMR ASSIGNMENTS

Ketopantoate reductase is an essential enzyme for pantothenate (vitamin B5) synthesis and a potential antibiotic target. Here we r..