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Research Output 1991 2019

2010
49 Citations (Scopus)

Sulfonamide linked neoglycoconjugates-A new class of inhibitors for cancer-associated carbonic anhydrases

Lopez, M., Bornaghi, L. F., Innocenti, A., Vullo, D., Charman, S. A., Supuran, C. T. & Poulsen, S-A., 2010, In : Journal of Medicinal Chemistry. 53, p. 2913 - 2926 14 p.

Research output: Contribution to journalArticleResearchpeer-review

54 Citations (Scopus)

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

10 Citations (Scopus)

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

75 Citations (Scopus)

The structure - activity relationship of the antimalarial ozonide arterolane (OZ277)

Dong, Y., Wittlin, S., Sriraghavan, K., Chollet, J., Charman, S. A., Charman, W. N., Scheurer, C., Urwyler, H., Santo Tomas, J., Snyder, C., Creek, D. J., Morizzi, J., Koltun, M., Matile, H., Wang, X., Padmanilayam, M., Tang, Y., Dorn, A., Brun, R. & Vennerstrom, J., 2010, In : Journal of Medicinal Chemistry. 53, p. 481 - 491 11 p.

Research output: Contribution to journalArticleResearchpeer-review

2009
2 Citations (Scopus)

2,5-Dimethyl-2,4-hexadiene induced photodechlorination of 9,10-dichloroanthracene

Saltiel, J., Smothers, W. K., Schanze, K. S., Charman, S. A. & Bonneau, R., 2009, In : Photochemical & Photobiological Sciences. 8, 6, p. 856 - 867 12 p.

Research output: Contribution to journalArticleResearchpeer-review

23 Citations (Scopus)

CYT997: a novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo

Burns, C., Fantino, E., Phillips, I. D., Su, S., Harte, M., Bukczynska, P. E., Frazzetto, M., Joffe, M., Kruszelnicki, I., Wang, B., Wang, Y., Wilson, N., Dilley, R. J., Wan, S. S., Charman, S. A., Shackleford, D., Fida, R., Malcontenti-Wilson, C. & Wilks, A. F., 2009, In : Molecular Cancer Therapeutics. 8, 11, p. 3036 - 3045 10 p.

Research output: Contribution to journalArticleResearchpeer-review

22 Citations (Scopus)

Discovery of CYT997: a structurally novel orally active microtubule targeting agent

Burns, C., Harte, M., Bu, X., Fantino, E., Joffe, M., Sikanyika, H., Su, S., Tranberg, C. E., Wilson, N., Charman, S. A., Shackleford, D. & Wilks, A. F., 2009, In : Bioorganic and Medicinal Chemistry Letters. 19, 16, p. 4639 - 4642 4 p.

Research output: Contribution to journalArticleResearchpeer-review

150 Citations (Scopus)

Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice

Gujjar, R., Marwaha, A., El Mazouni, F., White, J., White, K. L., Creason, S., Shackleford, D., Baldwin, J., Charman, W. N., Buckner, F. S., Charman, S. A., Rathod, P. & Phillips, M., 2009, In : Journal of Medicinal Chemistry. 52, 7, p. 1864 - 1872 9 p.

Research output: Contribution to journalArticleResearchpeer-review

50 Citations (Scopus)

Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs)

Burns, C., Bourke, D. G., Andrau, L., Bu, X., Charman, S. A., Donohue, A. C., Fantino, E., Farrugia, M., Feutrill, J. T., Joffe, M., Kling, R. M., Kurek, M., Nero, T. L., Nguyen, T., Palmer, J. T., Phillips, I. D., Shackleford, D., Sikanyika, H., Styles, M., Su, S. & 3 others, Treutlein, H. R., Zeng, J. & Wilks, A. F., 2009, In : Bioorganic and Medicinal Chemistry Letters. 19, 20, p. 5887 - 5892 6 p.

Research output: Contribution to journalArticleResearchpeer-review

40 Citations (Scopus)

S-glycosyl primary sulfonamides - A new structural class for selective inhibition of cancer-associated carbonic anhydrases

Lopez, M., Paul, B., Hofmann, A., Morizzi, J., Wu, Q. K., Charman, S. A., Innocenti, A., Vullo, D., Supuran, C. T. & Poulsen, S. A., 22 Oct 2009, In : Journal of Medicinal Chemistry. 52, 20, p. 6421-6432 12 p.

Research output: Contribution to journalArticleResearchpeer-review

6 Citations (Scopus)
21 Citations (Scopus)

Spiroadamantyl 1,2,4-trioxolane, 1,2,4-trioxane, and 1,2,4-trioxepane pairs: Relationship between peroxide bond iron(II) reactivity, heme alkylation efficiency, and antimalarial activity

Wang, X., Creek, D. J., Schiaffo, C. E., Dong, Y., Chollet, J., Scheurer, C., Wittlin, S., Charman, S. A., Dussault, P. H., Wood, J. K. & Vennerstrom, J., 2009, In : Bioorganic and Medicinal Chemistry Letters. 19, 16, p. 4542 - 4545 4 p.

Research output: Contribution to journalArticleResearchpeer-review

15 Citations (Scopus)

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
16 Citations (Scopus)
28 Citations (Scopus)

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

3 Citations (Scopus)

Pharmacokinetics and brain uptake of AM-36, a novel neuroprotective agent, following intravenous administration to rats

Nicolazzo, J., Nguyen, T. T., Katneni, K., Steuten, J. A., Smith, G. D., Jarrott, B., Callaway, J. K. & Charman, S. A., 2008, In : Journal of Pharmacy and Pharmacology. 60, 2, p. 171 - 178 8 p.

Research output: Contribution to journalArticleResearchpeer-review

500 Citations (Scopus)

Rapid restoration of cognition in alzheimer's transgenic mice with 8-hydroxy quinoline analogs is associated with decreased interstitial Abeta

Adlard, P. A., Cherny, R. A., Finklestein, D. I., Gautier, E., Robb, E., Cortes, M., Volitakis, I., Liu, X., Smith, J. P., Perez, K., Laughton, K. M., Lin, Q-X., Charman, S. A., Nicolazzo, J., Wilkins, S. J., Deleva, K., Lynch, T., Kok, G., Ritchie, C. W., Tanzi, R. E. & 4 others, Cappai, R., Masters, C. L., Barnham, K. J. & Bush, A. I., 2008, In : Neuron. 59, p. 43 - 55 13 p.

Research output: Contribution to journalArticleResearchpeer-review

77 Citations (Scopus)

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

11 Citations (Scopus)
2007
14 Citations (Scopus)

Comparative antimalarial activities of six pairs of 1,2,4,5-tetraoxanes (peroxide dimers) and 1,2,4,5,7,8-hexaoxonanes (peroxide trimers)

Dong, Y., Creek, D. J., Chollet, J., Matile, H., Charman, S. A., Wittlin, S., Woods, J. H. & Vennerstrom, J., 2007, In : Antimicrobial Agents and Chemotherapy. 51, 8, p. 3033 - 3035 3 p.

Research output: Contribution to journalArticleResearchpeer-review

47 Citations (Scopus)

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

41 Citations (Scopus)

Lymphatic absorption of subcutaneously administered proteins: influence of different injection sites on the absorption of darbepoetin alfa using a sheep model

Kota, J., Machavaram, K. K., McLennan, D. N., Edwards, G. A., Porter, C. J. & Charman, S. A., 2007, In : Drug Metabolism and Disposition. 35, 12, p. 2211 - 2217 7 p.

Research output: Contribution to journalArticleResearchpeer-review

42 Citations (Scopus)

Spiro- and dispiro-1,2-dioxolanes: contribution of iron(II)-mediated one-electron vs two-electron reduction to the activity of antimalarial peroxides

Wang, X., Dong, Y., Wittlin, S., Creek, D., Chollet, J., Charman, S. A., Santo Tomas, J., Scheurer, C., Snyder, C. & Vennerstrom, J., 2007, In : Journal of Medicinal Chemistry. 50, 23, p. 5840 - 5847 8 p.

Research output: Contribution to journalArticleResearchpeer-review

53 Citations (Scopus)

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
27 Citations (Scopus)

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

45 Citations (Scopus)

Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine

Padmanilayam, M., Scorneaux, B., Dong, Y., Chollet, J., Matile, H., Charman, S. A., Creek, D. J., Charman, W. N., Santo Tomas, J., Scheurer, C., Wittlin, S., Brun, R. & Vennerstrom, J., 2006, In : Bioorganic and Medicinal Chemistry Letters. 16, 21, p. 5542 - 5545 4 p.

Research output: Contribution to journalArticleResearchpeer-review

23 Citations (Scopus)

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

Contemporary bioequivalence issues for poorly water soluble drugs

Charman, W. N., Charman, S. A. & Porter, C. J. H., 2006, International Bioequivalence Standards: A New Era. Amidon, G., Lesko, L., Midha, K., Shah, V. & Hilfinger, J. (eds.). 1 ed. USA: TSRL Inc., Ann Arbor, p. 201 - 222 22 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Other

56 Citations (Scopus)

Effect of functional group polarity on the antimalarial activity of spiro and dispiro-1,2,4-trioxolanes

Dong, Y., Tang, Y., Chollet, J., Matile, H., Wittlin, S., Charman, S. A., Charman, W. N., Santo Tomas, J., Scheurer, C., Snyder, C., Scorneaux, B., Bajpai, S., Alexander, S. A., Wang, X., Padmanilayam, M., Cheruku, S. R., Brun, R. & Vennerstrom, J. L., 2006, In : Bioorganic & Medicinal Chemistry. 14, 18, p. 6368 - 6382 15 p.

Research output: Contribution to journalArticleResearchpeer-review

34 Citations (Scopus)

In vitro assessment of the pharmacodynamic properties and the partitioning of OZ277/RBx-11160 in cultures of Plasmodium falciparum

Maerki, S., Brun, R., Charman, S. A., Dorn, A., Matile, H. & Wittlin, S., 2006, In : Journal of Antimicrobial Chemotherapy. 58, 1, p. 52 - 58 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Lipid-based systems, drug exposure and lead optimization

Charman, W. N., Charman, S. A. & Porter, C. J. H., 2006, Optimizing the 'Drug-like' Properties of Leads in Drug Discovery. Borchardt, R. T., Kerns, E. H., Hageman, M. J., Thakker, D. R. & Stevens, J. L. (eds.). 1 ed. New York USA: Springer, p. 131 - 150 20 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

83 Citations (Scopus)

Methods to assess drug permeability across the blood-brain barrier

Nicolazzo, J. A., Charman, S. A. & Charman, W. N., 2006, In : Journal of Pharmacy and Pharmacology. 58, 3, p. 281 - 293 13 p.

Research output: Contribution to journalArticleResearchpeer-review

44 Citations (Scopus)

Permeability assessment of poorly water-soluble compounds under solubilizing conditions: the reciprocal permeability approach

Katneni, K., Charman, S. A. & Porter, C. J. H., 2006, In : Journal of Pharmaceutical Sciences. 95, 10, p. 2170 - 2185 16 p.

Research output: Contribution to journalArticleResearchpeer-review

25 Citations (Scopus)

The absorption of darbepoetin alfa occurs predominantly via the lymphatics following subcutaneous administration to sheep.

McLennan, D. N., Porter, C. J. H., Edwards, G. A., Heatherington, A. C., Martin, S. W. & Charman, S. A., 2006, In : Pharmaceutical Research. 23, 9, p. 2060 - 2066 7 p.

Research output: Contribution to journalArticleResearchpeer-review

31 Citations (Scopus)

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
34 Citations (Scopus)

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

42 Citations (Scopus)

Lymphatic absorption is the primary contributor to the systemic availability of epoetin alfa following subcutaneous administration to sheep

McLennan, D. N., Porter, C. J. H., Edwards, G. A., Martin, S. W., Heatherington, A. C. & Charman, S. A., 2005, In : Journal of Pharmacology and Experimental Therapeutics. 313, 1, p. 345 - 351 7 p.

Research output: Contribution to journalArticleResearchpeer-review

91 Citations (Scopus)

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

91 Citations (Scopus)

Subcutaneous drug delivery and the role of the lymphatics

McLennan, D. N., Porter, C. J. H. & Charman, S. A., 2005, In : Drug Discovery Today: Technologies. 2, 1, p. 89-96 8 p.

Research output: Contribution to journalArticleResearchpeer-review

2004
521 Citations (Scopus)

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

31 Citations (Scopus)

Pharmacokinetics of recombinant human leukemia inhibitory factor in sheep

Segrave, A. M., Mager, D. E., Charman, S. A., Edwards, G. & Porter, C. J. H., Jun 2004, In : Journal of Pharmacology and Experimental Therapeutics. 309, 3, p. 1085-1092 8 p.

Research output: Contribution to journalArticleResearchpeer-review

2003

Oral modified-release delivery systems

Charman, S. A. & Charman, W. N., 2003, Modified-Release Drug Delivery Technology. Rathbone, M. J., Hadgraft, J. & Roberts, M. S. (eds.). 1 ed. USA: Marcel Dekker, p. 1 - 10 10 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

31 Citations (Scopus)

Pharmacokinetic model to describe the lymphatic absorption of r-metHu-Leptin after subcutaneous injection to sheep

McLennan, D. N., Porter, C. J. H., Edwards, G. A., Brumm, M., Martin, S. W. & Charman, S. A., 1 Aug 2003, In : Pharmaceutical Research. 20, 8, p. 1156-1162 7 p.

Research output: Contribution to journalArticleResearchpeer-review

2002
22 Citations (Scopus)

Effect of dietary fatty acids on the intestinal permeability of marker drug compounds in excised rat jejunum

Vine, D. F., Charman, S. A., Gibson, P. R., Sinclair, A. J. & Porter, C. J. H., 2002, In : Journal of Pharmacy and Pharmacology. 54, 6, p. 809 - 819 11 p.

Research output: Contribution to journalArticleResearchpeer-review

2001
45 Citations (Scopus)

Lymphatic absorption is a significant contributor to the subcutaneous bioavailability of insulin in a sheep model

Charman, S. A., McLennan, D. N., Edwards, G. & Porter, C. J. H., 2001, In : Pharmaceutical Research. 18, 11, p. 1620-1626 7 p.

Research output: Contribution to journalArticleResearchpeer-review

78 Citations (Scopus)

Lymphatic transport of proteins after s.c. injection: Implications of animal model selection

Porter, C. J. H., Edwards, G. & Charman, S. A., 23 Aug 2001, In : Advanced Drug Delivery Reviews. 50, 1-2, p. 157-171 15 p.

Research output: Contribution to journalArticleResearchpeer-review

2000
168 Citations (Scopus)

Lymphatic transport of proteins after subcutaneous administration

Porter, C. J. H. & Charman, S. A., Mar 2000, In : Journal of Pharmaceutical Sciences. 89, 3, p. 297-310 14 p.

Research output: Contribution to journalArticleResearchpeer-review

70 Citations (Scopus)

Systemic availability and lymphatic transport of human growth hormone administered by subcutaneous injection

Charman, S. A., Segrave, A. M., Edwards, G. A. & Porter, C. J. H., Feb 2000, In : Journal of Pharmaceutical Sciences. 89, 2, p. 168-177 10 p.

Research output: Contribution to journalArticleResearchpeer-review

1999

A modified ussing chamber model for the evaluation of rhGH transepithelial absorption

McIntosh, K. A., Charman, W. N. & Charman, S. A., 1999, p. S-421 - S-421. 1 p.

Research output: Contribution to conferenceAbstract