20042019
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Research Output 2004 2019

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2019

3,3′-Disubstituted 5,5′-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity

Xue, L., Shi, D. H., Harjani, J. R., Huang, F., Beveridge, J. G., Dingjan, T., Ban, K., Diab, S., Duffy, S., Lucantoni, L., Fletcher, S., Chiu, F. C. K., Blundell, S., Ellis, K., Ralph, S. A., Wirjanata, G., Teguh, S., Noviyanti, R., Chavchich, M., Creek, D. & 10 others, Price, R. N., Marfurt, J., Charman, S. A., Cuellar, M. E., Strasser, J. M., Dahlin, J. L., Walters, M. A., Edstein, M. D., Avery, V. M. & Baell, J. B., 1 Jan 2019, In : Journal of Medicinal Chemistry. 62, 5, p. 2485-2498 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Potential Diagnostic Imaging of Alzheimer's Disease with Copper-64 Complexes That Bind to Amyloid-β Plaques

McInnes, L. E., Noor, A., Kysenius, K., Cullinane, C., Roselt, P., McLean, C. A., Chiu, F. C. K., Powell, A. K., Crouch, P. J., White, J. M. & Donnelly, P. S., 4 Mar 2019, In : Inorganic Chemistry. 58, 5, p. 3382-3395 14 p.

Research output: Contribution to journalArticleResearchpeer-review

2018

Using Human Plasma as an Assay Medium in Caco-2 Studies Improves Mass Balance for Lipophilic Compounds

Katneni, K., Pham, T., Saunders, J., Chen, G., Patil, R., White, K. L., Abla, N., Chiu, F. C. K., Shackleford, D. M. & Charman, S. A., 1 Nov 2018, In : Pharmaceutical Research. 35, 11, 13 p., 210.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
2017

Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439)

Dong, Y., Wang, X., Kamaraj, S., Bulbule, V. J., Chiu, F. C. K., Chollet, J., Dhanasekaran, M., Hein, C. D., Papastogiannidis, P., Morizzi, J., Shackleford, D. M., Barker, H., Ryan, E., Scheurer, C., Tang, Y., Zhao, Q., Zhou, L., White, K. L., Urwyler, H., Charman, W. N. & 4 others, Matile, H., Wittlin, S., Charman, S. A. & Vennerstrom, J. L., 13 Apr 2017, In : Journal of Medicinal Chemistry. 60, 7, p. 2654-2668 15 p.

Research output: Contribution to journalArticleResearchpeer-review

2016

A triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with improved drug-like properties for treatment and prevention of malaria

Phillips, M. A., White, K., Kokkonda, S., Deng, X., White, J., El Mazouni, F., Marsh, K., Tomchick, D. R., Manjalanagara, K., Rudra, K. R., Wirjanata, G., Noviyanti, R., Price, R. N., Marfurt, J., Shackleford, D., Chiu, F., Campbell, M., Jimenez-Diaz, M. B., Bazaga, S. F., Angulo-Barturen, I. & 1 others, Charman, S., 9 Dec 2016, In : ACS Infectious Diseases. 2, 12, p. 945-957 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Haemoglobin degradation underpins the sensitivity of early ring stage Plasmodium falciparum to artemisinins

Xie, S. C., Dogovski, C., Hanssen, E., Chiu, F., Yang, T., Crespo, M. P., Stafford, C., Batinovic, S., Teguh, S., Charman, S., Klonis, N. & Tilley, L., 2016, In : Journal of Cell Science. 129, 2, p. 406-416 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

Revisiting the SAR of the antischistosomal aryl hydantoin (Ro 13-3978)

Wang, C., Zhao, Q., Vargas, M., Jones, J. O., White, K., Shackleford, D., Chen, G., Saunders, J., Ng, A., Chiu, F., Dong, Y., Charman, S., Keiser, J. & Vennerstrom, J. L., 8 Dec 2016, In : Journal of Medicinal Chemistry. 59, 23, p. 10705-10718 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Understanding Oxadiazolothiazinone Biological Properties: Negative Inotropic Activity versus Cytochrome P450-Mediated Metabolism

Carosati, E., Cosimelli, B., Ioan, P., Severi, E., Katneni, K., Chiu, F. C. K., Saponara, S., Fusi, F., Frosini, M., Matucci, R., Micucci, M., Chiarini, A., Spinelli, D. & Budriesi, R., 28 Apr 2016, In : Journal of Medicinal Chemistry. 59, 7, p. 3340-3352 13 p.

Research output: Contribution to journalArticleResearchpeer-review

2015

Evidence for the in vitro bioactivation of aminopyrazole derivatives: trapping reactive aminopyrazole intermediates using glutathione ethyl ester in human liver microsomes

Ryan, E., Morrow, B. J., Hemley, C. F., Pinson, J-A., Charman, S. A., Chiu, F. C. K. & Foitzik, R. C., 2015, In : Chemical Research in Toxicology. 28, 9, p. 1747-1752 6 p.

Research output: Contribution to journalArticleResearchpeer-review

2013

Comparative antimalarial activities and ADME profiles of ozonides (1,2,4-trioxolanes) OZ277, OZ439, and their 1,2-dioxolane, 1,2,4-trioxane, and 1,2,4,5-tetraoxane isosteres

Wang, X., Dong, Y., Wittlin, S., Charman, S. A., Chiu, F. C. K., Chollet, J., Katneni, K., Mannila, J. M., Morizzi, J., Ryan, E., Scheurer, C., Steuten, J. A., Santo Tomas, J., Snyder, C. & Vennerstrom, J., 2013, In : Journal of Medicinal Chemistry. 56, 6, p. 2547 - 2555 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Two analogues of fenarimol show curative activity in an experimental model of chagas disease

Keenan, M., Chaplin, J. H., Alexander, P. W., Abbott, M. J., Best, W. M., Khong, A., Botero, A., Perez, C., Cornwall, S., Thompson, R. C. A., White, K. L., Shackleford, D., Koltun, M., Chiu, F. C. K., Morizzi, J., Ryan, E., Campbell, M., von Geldern, T. W., Scandale, I., Chatelain, E. & 1 others, Charman, S. A., 2013, In : Journal of Medicinal Chemistry. 56, 24, p. 10158 - 10170 13 p.

Research output: Contribution to journalArticleResearchpeer-review

2012

The hypoxia imaging agent Cu ii(atsm) is neuroprotective and improves motor and cognitive functions in multiple animal models of Parkinson's disease

Hung, L., Villemagne, V., Cheng, L., Sherratt, N., Ayton, S., White, A., Crouch, P., Lim, S. C., Leong, S. L., Wilkins, S., George, J., Roberts, B., Pham, C., Liu, X., Chiu, F., Shackleford, D., Powell, A., Masters, C., Bush, A. I., O'Keefe, G. & 7 others, Culvenor, J., Cappai, R., Cherny, R., Donnelly, P., Hill, A., Finkelstein, D. & Barnham, K., 2012, In : Journal of Experimental Medicine. 209, 4, p. 837 - 854 18 p.

Research output: Contribution to journalArticleResearchpeer-review

2011

Design, synthesis, and evaluation of a new fluorescent probe for measuring polymyxin-lipopolysaccharide binding interactions

Soon, R., Velkov, T., Chiu, F., Thompson, P., Kancharla, R., Roberts, K., Larson, I., Nation, R. & Li, J., 2011, In : Analytical Biochemistry. 409, 2, p. 273 - 283 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria

Charman, S., Arbe-Barnes, S., Bathurst, I., Brun, R., Campbell, M., Charman, W., Chiu, F., Chollet, J., Craft, C., Creek, D., Dong, Y., Matile, H., Maurer, M., Morizzi, J., Nguyen, T., Papastogiannidis, P., Scheurer, C., Shackleford, D., Sriraghavan, K., Stingelin, L. & 7 others, Tang, Y., Urwyler, H., Wang, X., White, K., Wittlin, S., Zhou, L. & Vennerstrom, J., 2011, In : Proceedings of the National Academy of Sciences. 108, 11, p. 4400 - 4405 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
2010

Synthesis and Biological Evaluation of Polysulfated Oligosaccharide Glycosides as Inhibitors of Angiogenesis and Tumor Growth

Johnstone, K. D., Karoli, T., Liu, L., Dredge, K., Copeman, E., Li, C. P., Davis, K., Hammond, E., Bytheway, I., Kostewicz, E. S., Chiu, F. C. K., Shackleford, D., Charman, S. A., Charman, W. N., Harenberg, J., Gonda, T. & Ferro, V., 2010, In : Journal of Medicinal Chemistry. 53, 4, p. 1686 - 1699 14 p.

Research output: Contribution to journalArticleResearchpeer-review

The comparative antimalarial properties of weak base and neutral synthetic ozonides

Tang, Y., Wittlin, S., Charman, S. A., Chollet, J., Chiu, F. C. K., Morizzi, J., Johnson, L., Santo Tomas, J., Scheurer, C., Snyder, C., Zhou, L., Dong, Y., Charman, W. N., Matile, H., Urwyler, H., Dorn, A. & Vennerstrom, J., 2010, In : Bioorganic and Medicinal Chemistry Letters. 20, 2, p. 563 - 566 4 p.

Research output: Contribution to journalArticleResearchpeer-review

2009

CpG methylation potentiates pixantrone and doxorubicin-induced DNA damage and is a marker of drug sensitivity

Evison, B. J., Bilardi, R. A., Chiu, F. C. K., Pezzoni, G., Phillips, D. R. & Cutts, S. M., 2009, In : Nucleic Acids Research. 37, 19, p. 6355 - 6370 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Stability of peroxide antimalarials in the presence of human hemoglobin

Creek, D. J., Ryan, E., Charman, W. N., Chiu, F. C. K., Prankerd, R., Vennerstrom, J. & Charman, S. A., 2009, In : Antimicrobial Agents and Chemotherapy. 53, 8, p. 3496 - 3500 5 p.

Research output: Contribution to journalArticleResearchpeer-review

2008

Characterization of the two major CYP450 metabolites of ozonide (1,2,4-trioxolane) OZ277

Zhou, L., Alker, A., Ruf, A., Wang, X., Chiu, F. C. K., Morizzi, J., Charman, S. A., Charman, W. N., Scheurer, C., Wittlin, S., Dong, Y., Hunziker, D. & Vennerstrom, J., 2008, In : Bioorganic and Medicinal Chemistry Letters. 18, 5, p. 1555 - 1558 4 p.

Research output: Contribution to journalArticleResearchpeer-review

Development and validation of a reversed-phase high-performance liquid chromatography assay for polymyxin B in human plasma

Cao, G., Ali, F. E. A., Chiu, F. C. K., Zavascki, A. P., Nation, R. L. & Li, J., 2008, In : Journal of Antimicrobial Chemotherapy. 62, 5, p. 1009 - 1014 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Formaldehyde-activated pixantrone is a monofunctional DNA alkylator that binds selectively to CpG and CpA doublets

Evison, B. J., Chiu, F. C. K., Pezzoni, G., Phillips, D. R. & Cutts, S. M., 2008, In : Molecular Pharmacology. 74, 1, p. 184 - 194 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Genistein- and daidzein 7-O-beta-D-glucuronic acid retain the ability to inhibit copper-mediated lipid oxidation of low density lipoprotein

Kgomotso, T., Chiu, F. C. K. & Ng, K., 2008, In : Molecular Nutrition and Food Research. 52, 12, p. 1457 - 1466 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Relationship between antimalarial activity and heme alkylation for spiro- and dispiro-1,2,4-trioxolane antimalarials

Creek, D. J., Charman, W. N., Chiu, F. C. K., Prankerd, R. J., Dong, Y., Vennerstrom, J. & Charman, S. A., 2008, In : Antimicrobial Agents and Chemotherapy. 52, 4, p. 1291 - 1296 6 p.

Research output: Contribution to journalArticleResearchpeer-review

2007

Identification and quantification of antioxidants in Fructus Lycii

Le, K., Chiu, F. C. K. & Ng, K. F., 2007, In : Food Chemistry. 105, 1, p. 353 - 363 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Iron-mediated degradation kinetics of substituted dispiro-1,2,4-trioxolane antimalarials

Creek, D. J., Charman, W. N., Chiu, F. C. K., Prankerd, R. J., McCullough, K. J., Dong, Y., Vennerstrom, J. & Charman, S. A., 2007, In : Journal of Pharmaceutical Sciences. 96, 11, p. 2945 - 2956 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Weak base dispiro-1,2,4-trioxolanes: potent antimalarial ozonides

Tang, Y., Dong, Y., Wittlin, S., Charman, S. A., Chollet, J., Chiu, F. C. K., Charman, W. N., Matile, H., Urwyler, H., Dorn, A., Bajpai, S., Wang, X., Padmanilayam, M., Karle, J. M., Brun, R. & Vennerstrom, J., 2007, In : Bioorganic and Medicinal Chemistry Letters. 17, 5, p. 1260 - 1265 6 p.

Research output: Contribution to journalArticleResearchpeer-review

2006

Alteration of the intravenous pharmacokinetics of a synthetic ozonide antimalarial in the presence of a modified cyclodextrin

Charman, S. A., Perry, C. S., Chiu, F. C. K., McIntosh, K. A., Prankerd, R. J. & Charman, W. N., 2006, In : Journal of Pharmaceutical Sciences. 95, 2, p. 256 - 267 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Chemical kinetics and aqueous degradation pathways of a new class of synthetic ozonide antimalarials

Perry, C. S., Charman, S. A., Prankerd, R. J., Chiu, F. C. K., Dong, Y., Vennerstrom, J. L. & Charman, W. N., 2006, In : Journal of Pharmaceutical Sciences. 95, 4, p. 737 - 747 11 p.

Research output: Contribution to journalArticleResearchpeer-review

The binding interaction of synthetic ozonide antimalarials with natural and modified beta-cyclodextrins

Perry, C. S., Charman, S. A., Prankerd, R. J., Chiu, F. C. K., Scanlon, M. J., Chalmers, D. K. & Charman, W. N., 2006, In : Journal of Pharmaceutical Sciences. 95, 1, p. 146 - 158 13 p.

Research output: Contribution to journalArticleResearchpeer-review

2005

Kinetics of iron-mediated artemisinin degradation: effect of solvent composition and iron salt

Creek, D. J., Chiu, F. C. K., Prankerd, R. J., Charman, S. A. & Charman, W. N., 2005, In : Journal of Pharmaceutical Sciences. 94, 8, p. 1820 - 1829 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes

Dong, Y., Chollet, J., Matile, H., Charman, S. A., Chiu, F. C. K., Charman, W. N., Scorneaux, B., Urwyler, H., Santo Tomas, J., Scheurer, C., Snyder, C., Dorn, A., Wang, X., Karle, J. M., Tang, Y., Wittlin, S., Brun, R. & Vennerstrom, J. L., 2005, In : Journal of Medicinal Chemistry. 48, 15, p. 4953 - 4961 9 p.

Research output: Contribution to journalArticleResearchpeer-review

2004

Identification of an antimalarial synthetic trioxolane drug development candidate

Vennerstrom, J. L., Arbe-Barnes, S., Brun, R., Charman, S. A., Chiu, F. C. K., Chollet, J., Dong, Y., Dorn, A., Hunziker, D., Matile, H., McIntosh, K. A., Padmanilayam, M., Santo Tomas, J., Scheurer, C., Scorneaux, B., Tang, Y., Urwyler, H., Wittlin, S. & Charman, W. N., 19 Aug 2004, In : Nature. 430, 7002, p. 900-904 5 p.

Research output: Contribution to journalArticleResearchpeer-review