Dr Jennifer Baker
Postdoctoral Researcher
School of Environmental and Life Sciences (Chemistry)
Career Summary
Biography
Receiving undergraduate qualifications in Science from the University of Newcastle in 2014. Jennifer continued on to an Honours degree in Chemistry, graduating in 2016 with Honours Class I. Undertaking a PhD in Medicinal Chemistry, she completed this under the supervision of Prof. Adam McCluskey and Dr. Jennette Sakoff in 2020.
Beginning work as a post-doctoral researcher immediately upon completing her doctorate, Jennifer's interest lies primarily in the development of small molecules for various anti-cancer targets, particularly with the use of in silico modelling techniques for drug design. Additionally, she has a keen interest in the use of Flow Chemistry methodologies for both the synthesis and scale-up of biologically active small molecules. Jennifer is primarily involved with developing small molecules that target the histone demethylase KDM4, as well as the Arylhydrocarbon Receptor, a nuclear translocator that has been associated with breast cancer.
In addition to Jennifer's research, she has been involved in a number of different teaching roles, including the annual outreach events hosted by the School of Environmental and Life Sciences for high school students, Experiment Fest and ASSETS (co-hosted by CSIRO). She has also been involved in lecture and course-coordination roles for the University of Newcastle's enabling programs. Jennifer has also lectured the 1st-year introductory Chemistry courses CHEM1010 and CHEM1120, and the 3rd year CHEM3550 (Medicinal and Biological Chemistry).
Qualifications
- Doctor of Philosophy, University of Newcastle
- Bachelor of Science (Chemistry), University of Newcastle
- Bachelor of Science (Honours), University of Newcastle
Keywords
- Computational Biological Chemistry
- Drug Design
- Medicinal Chemistry
- Molecular Modelling
- Organic Chemistry
Languages
- English (Mother)
Fields of Research
Code | Description | Percentage |
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340499 | Medicinal and biomolecular chemistry not elsewhere classified | 35 |
340599 | Organic chemistry not elsewhere classified | 35 |
340701 | Computational chemistry | 30 |
Professional Experience
UON Appointment
Title | Organisation / Department |
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Postdoctoral Researcher | University of Newcastle School of Environmental and Life Sciences Australia |
Casual Academic - Open Foundation | University of Newcastle Learning and Teaching Australia |
Teaching
Code | Course | Role | Duration |
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CHEM1010 |
Introductory Chemistry I College of Engineering, Science and Environment, University of Newcastle |
Conducted the lectures and tutorials for the Organic Chemistry component of this course. | 1/1/2021 - 28/2/2021 |
CHEM1120 |
Chemistry for the Life Sciences II College of Engineering, Science and Environment, University of Newcastle This course is the second of two foundational Chemistry (the Central Science) courses, giving students from a wide range of programs the required background to move on to degrees within the science, engineering, human nutrition and life sciences. |
Conducted the lectures and tutorials for the Concepts in Bioorganic Chemistry section of this course. | 1/8/2021 - 30/11/2021 |
CHEM1010 |
Introductory Chemistry I College of Engineering, Science and Environment, University of Newcastle This course is designed to give students from a wide range of programs the Chemistry (the Central Science) required to move on to various degrees within the science, engineering and life sciences. |
Conducted the lectures and tutorials for the Organic Chemistry component of this course. | 1/6/2020 - 31/7/2020 |
CHEM1010 |
Introductory Chemistry I College of Engineering, Science and Environment, University of Newcastle |
Conducted the lectures and tutorials for the Organic Chemistry component of this course. | 1/6/2021 - 31/7/2021 |
CHEM3550 |
Medicinal and Biological Chemistry College of Engineering, Science and Environment, University of Newcastle This course covers the biology, as well as the synthetic and structural chemistry, behind both current and emerging medicinal agents. |
Designed, generated and delivered an all-new teaching and laboratory module in Computer-Aided Drug Design for this advanced organic and medicinal chemistry course. | 1/8/2021 - 30/11/2021 |
CHEM1010 |
Introductory Chemistry I College of Engineering, Science & Environment, University of Newcastle |
Lecturer/Course Coordinator | 9/1/2023 - 10/2/2023 |
Publications
For publications that are currently unpublished or in-press, details are shown in italics.
Chapter (3 outputs)
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2022 |
Baker J, McCluskey A, Russell C, '8.08 - 1,3-Thiazines and Their Benzo Derivatives', Comprehensive Heterocyclic Chemistry IV: Volume 8: Six-membered Rings with Two Heteroatoms, and their Fused Carbocyclic Derivatives, Elsevier Science, Amsterdam, Netherlands 583-634 (2022)
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2019 |
Paula S, Baker JR, Zhu X, McCluskey A, 'Binding of chlorinated phenylacrylonitriles to the aryl hydrocarbon receptor: computational docking and molecular dynamics simulations', Molecular Docking and Molecular Dynamics, Intech Open, Rijeka 7-18 (2019) [B1]
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2017 |
Russell C, Baker JR, Cossar P, McCluskey A, 'Recent Developments in the Use of Flow Hydrogenation in the Field of Medicinal Chemistry', New Advances in Hydrogenation Processes - Fundamentals and Applications, InTech, London (2017)
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Journal article (26 outputs)
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2023 |
Cossar PJ, Cardoso D, Mathwin D, Russell CC, Chiew B, Hamilton MP, et al., 'Wiskostatin and other carbazole scaffolds as off target inhibitors of dynamin I GTPase activity and endocytosis', European Journal of Medicinal Chemistry, 247 (2023) [C1] Wiskostatin (1-(3,6-dibromo-9H-carbazol-9-yl)-3-(dimethylamino)propan-2-ol) (1) is a carbazole-based compound reported as a specific and relatively potent inhibitor of the N-WASP ... [more] Wiskostatin (1-(3,6-dibromo-9H-carbazol-9-yl)-3-(dimethylamino)propan-2-ol) (1) is a carbazole-based compound reported as a specific and relatively potent inhibitor of the N-WASP actin remodelling complex (S-isomer EC50 = 4.35 µM; R-isomer EC50 = 3.44 µM). An NMR solution structure showed that wiskostatin interacts with a cleft in the regulatory GTPase binding domain of N-WASP. However, numerous studies have reported wiskostatin's actions on membrane transport and cytokinesis that are independent of the N-WASP-Arp2/3 complex pathway, but offer limited alternative explanation. The large GTPase, dynamin has established functional roles in these pathways. This study reveals that wiskostatin and its analogues, as well as other carbazole-based compounds, are inhibitors of helical dynamin GTPase activity and endocytosis. We characterise the effects of wiskostatin on in vitro dynamin GTPase activity, in-cell endocytosis, and determine the importance of wiskostatin functional groups on these activities through design and synthesis of libraries of wiskostatin analogues. We also examine whether other carbazole-based scaffolds frequently used in research or the clinic also modulate dynamin and endocytosis. Understanding off-targets for compounds used as research tools is important to be able to confidently interpret their action on biological systems, particularly when the target and off-targets affect overlapping mechanisms (e.g. cytokinesis and endocytosis). Herein we demonstrate that wiskostatin is a dynamin inhibitor (IC50 20.7 ± 1.2 µM) and a potent inhibitor of clathrin mediated endocytosis (IC50 = 6.9 ± 0.3 µM). Synthesis of wiskostatin analogues gave rise to 1-(9H-carbazol-9-yl)-3-((4-methylbenzyl)amino)propan-2-ol (35) and 1-(9H-carbazol-9-yl)-3-((4-chlorobenzyl)amino)propan-2-ol (43) as potent dynamin inhibitors (IC50 = 1.0 ± 0.2 µM), and (S)-1-(3,6-dibromo-9H-carbazol-9-yl)-3-(dimethylamino)propan-2-ol (8a) and (R)-1-(3,6-dibromo-9H-carbazol-9-yl)-3-(dimethylamino)propan-2-ol (8b) that are amongst the most potent inhibitors of clathrin mediated endocytosis yet reported (IC50 = 2.3 ± 3.3 and 2.1 ± 1.7 µM, respectively).
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2023 |
Sun J, Baker JR, Russell CC, Pham HNT, Goldsmith CD, Cossar PJ, et al., 'Novel piperazine-1,2,3-triazole leads for the potential treatment of pancreatic cancer', RSC Medicinal Chemistry, 14 2246-2267 [C1]
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2023 |
Sterling J, Baker JR, McCluskey A, Munoz L, 'Systematic literature review reveals suboptimal use of chemical probes in cell-based biomedical research.', Nat Commun, 14 3228 (2023) [C1]
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2022 |
Sun J, Ambrus JI, Baker JR, Russell CC, Cossar PJ, Sakoff JA, et al., '3,5-Bis(trifluoromethyl)phenylsulfonamides, a novel pancreatic cancer active lead. Investigation of the terminal aromatic moiety.', Bioorg Med Chem Lett, 61 128591 (2022) [C1]
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2022 |
Prichard KL, O'Brien NS, Murcia SR, Baker JR, McCluskey A, 'Role of Clathrin and Dynamin in Clathrin Mediated Endocytosis/Synaptic Vesicle Recycling and Implications in Neurological Diseases', FRONTIERS IN CELLULAR NEUROSCIENCE, 15 (2022) [C1]
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2022 |
Stevens AJ, Abraham R, Young KA, Russell CC, McCluskey SN, Baker JR, et al., 'Antigiardial Activity of Novel Guanidine Compounds', CHEMMEDCHEM, 17 (2022) [C1]
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2022 |
Baker JR, Cossar PJ, Blaskovich MAT, Elliott AG, Zuegg J, Cooper MA, et al., 'Amino Alcohols as Potential Antibiotic and Antifungal Leads', Molecules, 27 (2022) [C1] Five focused compound libraries (forty-nine compounds), based on prior studies in our laboratory were synthesized and screened for antibiotic and anti-fungal activity against S. a... [more] Five focused compound libraries (forty-nine compounds), based on prior studies in our laboratory were synthesized and screened for antibiotic and anti-fungal activity against S. aureus, E. coli, K. pneumoniae, P. aeruginosa, A. baumannii, C. albicans and C. neoformans. Low levels of activity, at the initial screening concentration of 32 µg/mL, were noted with analogues of (Z)-2-(3,4-dichlorophenyl)-3-phenylacrylonitriles which made up the first two focused libraries produced. The most promising analogues possessing additional substituents on the terminal aromatic ring of the synthesised acrylonitriles. Modifications of the terminal aromatic moiety were explored through epoxide installation flowed by flow chemistry mediated ring opening aminolysis with discreet sets of amines to the corresponding amino alcohols. Three new focused libraries were developed from substituted anilines, cyclic amines, and phenyl linked heterocyclic amines. The aniline-based compounds were inactive against the bacterial and fungal lines screened. The introduction of a cyclic, such as piperidine, piperazine, or morpholine, showed >50% inhibition when evaluated at 32 µg/mL compound concentration against methicillin-resistant Staphylococcus aureus. Examination of the terminal aromatic substituent via oxirane aminolysis allowed for the synthesis of three new focused libraries of afforded amino alcohols. Aromatic substituted piperidine or piperazine switched library activity from antibacterial to anti-fungal activity with ((Z)-2-(3,4-dichlorophenyl)-3-(4-(2-hydroxy-3-(4-methylpiperazin-1-yl)propoxy)phenyl)acrylonitrile), ((Z)-2-(3,4-dichlorophenyl)-3-(4-(2-hydroxy-3-(4-(4-hydroxyphenyl)piperazin-1-yl)propoxy)-phenyl)acrylonitrile) and ((Z)-3-(4-(3-(4-cyclohexylpiperazin-1-yl)-2-hydroxypropoxy)-phenyl)-2-(3,4-dichlorophenyl)-acrylonitrile) show-ing >95% inhibition of Cryptococcus neoformans var. grubii H99 growth at 32 µg/mL. While (Z)-3-(4-(3-(cyclohexylamino)-2-hydroxypropoxy)phenyl)-2-(3,4-dichlorophenyl)-acrylonitrile, (S,Z)-2-(3,4-dichlorophenyl)-3-(4-(2-hydroxy-3-(piperidin-1-yl)propoxy)phenyl)acrylonitrile, (R,Z)-2-(3,4-dichlorophenyl)-3-(4-(2-hydroxy-3-(piperidin-1-yl)propoxy)phenyl)acrylonitrile, (Z)-2-(3,4-dichloro-phenyl)-3-(4-(2-hydroxy-3-(D-11-piperidin-1-yl)propoxy)phenyl)-acrylonitrile, and (Z)-3-(4-(3-(4-cyclo-hexylpiperazin-1-yl)-2-hydroxypropoxy)-phenyl)-2-(3,4-dichlorophenyl)-acrylonitrile 32 µg/mL against Staphylococcus aureus.
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2022 |
Zhang Q, Kounde CS, Mondal M, Greenfield JL, Baker JR, Kotelnikov S, et al., 'Light-mediated multi-target protein degradation using arylazopyrazole photoswitchable PROTACs (AP- PROTACs)', CHEMICAL COMMUNICATIONS, 58 10933-10936 (2022) [C1]
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2021 |
Baker JR, Russell CC, Gilbert J, McCluskey A, Sakoff JA, 'Amino alcohol acrylonitriles as broad spectrum and tumour selective cytotoxic agents', RSC MEDICINAL CHEMISTRY, 12 929-+ (2021) [C1]
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2021 |
Baker JR, Pollard BL, Lin AJS, Gilbert J, Paula S, Zhu X, et al., 'Modelling and Phenotypic Screening of NAP-6 and 10-Cl-BBQ, AhR Ligands Displaying Selective Breast Cancer Cytotoxicity in Vitro', CHEMMEDCHEM, 16 1499-1512 (2021) [C1]
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2021 |
Sun J, Ambrus JI, Russell CC, Baker JR, Cossar PJ, Pirinen MJ, et al., 'Targeting the S100A2-p53 Interaction with a Series of 3,5-Bis(trifluoromethyl)benzene Sulfonamides: Synthesis and Cytotoxicity', ChemMedChem, 16 2851-2863 (2021) [C1] In silico approaches identified 1, N-(6-((4-bromo- benzyl)amino)hexyl)-3,5-bis(trifluoromethyl)benzene sulfonamide, as a potential inhibitor of the S100A2-p53 protein-protein inte... [more] In silico approaches identified 1, N-(6-((4-bromo- benzyl)amino)hexyl)-3,5-bis(trifluoromethyl)benzene sulfonamide, as a potential inhibitor of the S100A2-p53 protein-protein interaction, a validated pancreatic cancer drug target. Subsequent cytotoxicity screening revealed it to be a 2.97 µM cell growth inhibitor of the MiaPaCa-2 pancreatic cell line. This is in keeping with our hypothesis that inhibiting this interaction would have an anti-pancreatic cancer effect with S100A2, the validated PC drug target. A combination of focused library synthesis (three libraries, 24 compounds total) and cytotoxicity screening identified a propyl alkyl diamine spacer as optimal; the nature of the terminal phenyl substituent had limited impact on observed cytotoxicity, whereas N-methylation was detrimental to activity. In total 15 human cancer cell lines were examined, with most analogues showing broad-spectrum activity. Near uniform activity was observed against a panel of six pancreatic cancer cell lines: MiaPaCa-2, BxPC-3, AsPC-1, Capan-2, HPAC and PANC-1. In all cases there was good to excellent correlation between the predicted docking pose in the S100A2-p53 binding groove and the observed cytotoxicity, especially in the pancreatic cancer cell line with high endogenous S100A2 expression. This supports S100A2 as a pancreatic cancer drug target.
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2021 |
Sun J, Baker JR, Russell CC, Cossar PJ, Ngoc Thuy Pham H, Sakoff JA, et al., 'Cytotoxic 1,2,3-Triazoles as Potential Leads Targeting the S100A2-p53 Complex: Synthesis and Cytotoxicity', ChemMedChem, 16 2864-2881 (2021) [C1] In silico screening predicted 1 (N-(4-((4-(3-(4-(3-methoxyphenyl)-1H-1,2,3-triazol-1-yl)propyl)piperazin-1-yl) sulfonyl)-phenyl)acetamide) as an inhibitor of the S100A2-p53 protei... [more] In silico screening predicted 1 (N-(4-((4-(3-(4-(3-methoxyphenyl)-1H-1,2,3-triazol-1-yl)propyl)piperazin-1-yl) sulfonyl)-phenyl)acetamide) as an inhibitor of the S100A2-p53 protein-protein interaction. S100A2 is a validated pancreatic cancer drug target. In the MiaPaCa-2 pancreatic cell line, 1 was a ~50 µM growth inhibitor. Synthesis of five focused compound libraries and cytotoxicity screening revealed increased activity from the presence of electron withdrawing moieties on the sulfonamide aromatic ring, with the 3,5-bis-CF3 Library 3 analogues the most active, with GI50 values of 0.91 (3-ClPh; 13 i; BxPC-3, Pancreas) to 9.0 µM (4-CH3; 13 d; PANC-1, Pancreas). Activity was retained against an expanded pancreatic cancer cell line panel (MiaPaCa-2, BxPC-3, AsPC-1, Capan-2, PANC-1 and HPAC) and the normal cell line MCF10A (breast). Bulky 4-disposed substituents on the terminal phenyl ring enhanced broad spectrum activity with growth inhibition values spanning 1.1 to 3.1 µM (4-C(CH3)3; 13 e; BxPC-3 and AsPC-1 (pancreas), respectively). Central alkyl spacer contraction from propyl to ethyl proved detrimental to activity with Library 4 and 5.5- to 10-fold less cytotoxic than the propyl linked Library 2 and Library 3. The data herein was consistent with the predicted binding poses of the compounds evaluated. The highest levels of cytotoxicity were observed with those analogues best capable of adopting a near identical pose to the p53-peptide in the S100A2-p53 binding groove.
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2021 |
Stanton DT, Baker JR, McCluskey A, Paula S, 'Development and interpretation of a QSAR model for in vitro breast cancer (MCF-7) cytotoxicity of 2-phenylacrylonitriles', Journal of Computer-Aided Molecular Design, 35 613-628 (2021) [C1] The Arylhydrocarbon Receptor (AhR), a member of the Per-ARNT-SIM transcription factor family, has been as a potential new target to treat breast cancer sufferers. A series of 2-ph... [more] The Arylhydrocarbon Receptor (AhR), a member of the Per-ARNT-SIM transcription factor family, has been as a potential new target to treat breast cancer sufferers. A series of 2-phenylacrylonitriles targeting AhR has been developed that have shown promising and selective activity against cancerous cell lines while sparing normal non-cancerous cells. A quantitative structure¿activity relationship (QSAR) modeling approach was pursued in order to generate a predictive model for cytotoxicity to support ongoing synthetic activities and provide important structure-activity information for new structure design. Recent work conducted by us has identified a number of compounds that exhibited false positive cytotoxicity values in the standard MTT assay. This work describes a good quality model that not only predicts the activity of compounds in the MCF-7 breast cancer cell line, but was also able to identify structures that subsequently gave false positive values in the MTT assay by identifying compounds with aberrant biological behavior. This work not only allows the design of future breast cancer cytotoxic activity in vitro, but allows the avoidance of the synthesis of those compounds anticipated to result in anomalous cytotoxic behavior, greatly enhancing the design of such compounds.
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2020 |
Baker JR, Russell CC, Gilbert J, Sakoff JA, McCluskey A, 'Amino Alcohol Acrylonitriles as Activators of the Aryl Hydrocarbon Receptor Pathway: An Unexpected MTT Phenotypic Screening Outcome', ChemMedChem, 15 490-505 (2020) [C1]
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2020 |
Pi H, Hang TN, Venter H, Boileau AR, Woolford L, Garg S, et al., 'In vitroActivity of Robenidine Analog NCL195 in Combination With Outer Membrane Permeabilizers Against Gram-Negative Bacterial Pathogens and Impact on Systemic Gram-Positive Bacterial Infection in Mice', Frontiers in Microbiology, 11 (2020) [C1]
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2020 |
Baker JR, Sakoff JA, McCluskey A, 'The aryl hydrocarbon receptor (AhR) as a breast cancer drug target', Medicinal Research Reviews, 40 972-1001 (2020) [C1]
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2019 |
Russell CC, Stevens A, Young KA, Baker JR, McCluskey SN, Khazandi M, et al., 'Discovery of 4,6-bis(2-((E)-benzylidene)hydrazinyl)pyrimidin-2-Amine with Antibiotic Activity.', ChemistryOpen, 8 896-907 (2019) [C1]
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2018 |
Baker JR, Gilbert J, Paula S, Zhu X, Sakoff JA, McCluskey A, 'Dichlorophenylacrylonitriles as AhR Ligands That Display Selective Breast Cancer Cytotoxicity in vitro', CHEMMEDCHEM, 13 1447-1458 (2018) [C1]
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2018 |
Cossar PJ, Baker JR, Cain N, McCluskey A, 'In situ epoxide generation by dimethyldioxirane oxidation and the use of epichlorohydrin in the flow synthesis of a library of beta-amino alcohols', ROYAL SOCIETY OPEN SCIENCE, 5 (2018) [C1]
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2018 |
Ghods A, Gilbert J, Baker JR, Russell CC, Sakoff JA, McCluskey A, 'A focused library synthesis and cytotoxicity of quinones derived from the natural product bolinaquinone', Royal Society Open Science, 5 (2018) [C1] Bolinaquinone is a natural product that is a structurally complex, cytotoxic sesquiterpene quinone. A scaffold simplification and focused library approach using a microwave-assist... [more] Bolinaquinone is a natural product that is a structurally complex, cytotoxic sesquiterpene quinone. A scaffold simplification and focused library approach using a microwave-assisted Suzuki coupling gave 32 bolinaquinone analogues with good-to-excellent cytotoxicity profiles. Mono-arylbenzoquinones, Library A, were preferentially toxic towards BE2-C (neuroblastoma) cells with growth inhibition (GI50) values of 4¿12 µM; only the 3,4-dimethoxyphenyl 23 and 3-biphenyl 28 variants were broad-spectrum active¿HT29 (colon carcinoma), U87 and SJ-G2 (glioblastoma), MCF-7 (breast carcinoma), A2780 (ovarian carcinoma), H460 (lung carcinoma), A431 (skin carcinoma), Du145 (prostate carcinoma), BE2-C (neuroblastoma), MIA (pancreatic carcinoma) and SMA (spontaneous murine astrocytoma). Library B with a second aryl moiety exhibited broad-spectrum cytotoxicity with MCF-7 cells¿ GI50 values of 5.6 ± 0.7 and 5.1 ± 0.5 µM for 2,5-dimethoxy-3-(naphthalene-1-yl)-6-(naphthalene-3-yl) 33 and 2,5-dimethoxy-3-(biaryl-2-yl)-6-(naphthalene-3-yl) 36, respectively. Similar potencies were also noted with 2,5-dimethoxy-3,6-diphenyl 30 against A2780 (GI50 = 5.9 ± 0.0 µM) and with 2,5-dimethoxy-3-(biaryl-3-yl)-6-(naphthalene-3-yl) 37 against HT29 (GI50 = 5.4 ± 0.4 µM), while the 3,4-dimethoxy mono-aryl analogue 23 exhibited good levels of activity against A2780 (GI50 = 3.8 ± 0.75 µM), the neuroblastoma cell line BE2-C (GI50 = 3 ± 0.35 µM) and SMA (GI50 = 3.9 ± 0.54 µM). Introduction of the amino-substituted Library C gave 2-(naphthalen-1-yl)-5-(naphthalen-3-yl)-3,6-bis(propylamino) 43, with excellent activity against HT29 (0.08 ± 0.0 µM), MCF-7 (0.17 ± 0.1 µM), A2780 (0.14 ± 0.1 µM), A431 (0.11 ± 0.0 µM), Du145 (0.16 ± 0.1 µM), BE2-C (0.08 ± 0.0 µM) and MIA (0.1 ± 0.0 µM).
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2018 |
Russell CC, Stevens A, Pi H, Khazandi M, Ogunniyi AD, Young KA, et al., 'Gram-Positive and Gram-Negative Antibiotic Activity of Asymmetric and Monomeric Robenidine Analogues', CHEMMEDCHEM, 13 2573-2580 (2018) [C1]
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2016 |
Robertson MJ, Horatscheck A, Sauer S, von Kleist L, Baker JR, Stahlschmidt W, et al., '5-Aryl-2-(naphtha-1-yl)sulfonamido-thiazol-4(5
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2016 |
Lin AJS, Russell CC, Baker JR, Frailey SL, Sakoff JA, McCluskey A, 'A facile hybrid 'flow and batch' access to substituted 3,4-dihydro-2: H -benzo [b] [1,4]oxazinones', Organic and Biomolecular Chemistry, 14 8732-8742 (2016) [C1] We describe a simple flow chemistry approach to libraries of ethyl 3-oxo-2-(substituted-phenylamino)-3,4-dihydro-2H-benzo[b][1,4]oxazine-6-carboxylates (12a-l) and N-ethyl-3-oxo-2... [more] We describe a simple flow chemistry approach to libraries of ethyl 3-oxo-2-(substituted-phenylamino)-3,4-dihydro-2H-benzo[b][1,4]oxazine-6-carboxylates (12a-l) and N-ethyl-3-oxo-2-(substituted-phenylamino)-3,4-dihydro-2H-benzo[b][1,4]oxazine-6-carboxamides (13a-l) in 38-87% yields. This scaffold is poorly described in the chemical literature. Screening against a panel of 11 cancer and one normal cell line showed that the amide linked library 13a-l was devoid of toxicity. Whereas the ester linked analogues 12b, 12c, 12g, 12j and 12l were highly cytotoxic with growth inhibition (GI50) values from 0.34 to >50 µM across all cell lines, with the 2-OH-Ph substituted 12l analogue presenting with sub-micromolar potency against the A2780 (ovarian; 0.34 ± 0.04 µM), BEC-2 (glioblastoma; 0.35 ± 0.06 µM), MIA (pancreas; 0.91 ± 0.054 µM) and SMA (murine glioblastoma; 0.77 ± 0.029 µM) carcinoma cell lines. Interestingly, the U87 glioblastoma cell line showed inherent resistance to growth inhibition by all analogues (GI50 32 to >50 µM) while the A2780 cells were highly sensitive (GI50 3.8-0.34 µM), suggesting that the analogues developed herein may be valuable lead compounds for the development of ovarian carcinoma specific cytotoxic agents. The differences in amide versus ester cytotoxicity was consitent with esterase cleaveage to release the cytotoxic warhead.
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Show 23 more journal articles |
Conference (1 outputs)
Year | Citation | Altmetrics | Link | ||
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2020 |
Sakoff J, Gilbert J, Baker J, McCluskey A, 'The aryl hydrocarbon receptor pathway and breast cancer', ASIA-PACIFIC JOURNAL OF CLINICAL ONCOLOGY (2020)
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Grants and Funding
Summary
Number of grants | 16 |
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Total funding | $452,064 |
Click on a grant title below to expand the full details for that specific grant.
Highlighted grants and funding
Fulbright Postdoctoral Fellowship$32,500
Funding body: Australian-American Fulbright Association
Funding body | Australian-American Fulbright Association |
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Scheme | Postdoctoral Scholarship |
Role | Lead |
Funding Start | 2024 |
Funding Finish | 2024 |
GNo | |
Type Of Funding | C1700 - Aust Competitive - Other |
Category | 1700 |
UON | N |
Developing novel agents to prevent tumour recurrence in glioblastoma$312,000
Funding body: NHMRC (National Health & Medical Research Council)
Funding body | NHMRC (National Health & Medical Research Council) |
---|---|
Project Team | Doctor Jennifer Baker, Associate Professor Lenka Munoz, Professor Terrance Johns |
Scheme | Ideas Grants |
Role | Lead |
Funding Start | 2021 |
Funding Finish | 2023 |
GNo | G2100506 |
Type Of Funding | C1100 - Aust Competitive - NHMRC |
Category | 1100 |
UON | Y |
20241 grants / $32,500
Fulbright Postdoctoral Fellowship$32,500
Funding body: Australian-American Fulbright Association
Funding body | Australian-American Fulbright Association |
---|---|
Scheme | Postdoctoral Scholarship |
Role | Lead |
Funding Start | 2024 |
Funding Finish | 2024 |
GNo | |
Type Of Funding | C1700 - Aust Competitive - Other |
Category | 1700 |
UON | N |
20224 grants / $28,821
Novel anti-infective agents$14,950
Funding body: College of Engineering, Science and Environment, University of Newcastle
Funding body | College of Engineering, Science and Environment, University of Newcastle |
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Project Team | Professor Adam McCluskey, Dr Beatrice Chiew |
Scheme | CESE Industry Matched Funding Scheme |
Role | Lead |
Funding Start | 2022 |
Funding Finish | 2022 |
GNo | |
Type Of Funding | Internal |
Category | INTE |
UON | N |
Machine learning for the design of novel small molecules to inhibit KDM4A as an anti-cancer target$7,320
Funding body: College of Engineering, Science and Environment, University of Newcastle
Funding body | College of Engineering, Science and Environment, University of Newcastle |
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Scheme | Fellowship Accelerator Scheme |
Role | Lead |
Funding Start | 2022 |
Funding Finish | 2022 |
GNo | |
Type Of Funding | Internal |
Category | INTE |
UON | N |
Closing the gap: Enhancing the first-year experience in Chemistry courses, creating successful transitions from enabling to undergraduate study$4,387
Funding body: Pathways and Academic Learning Support Centre Small Grants Scheme
Funding body | Pathways and Academic Learning Support Centre Small Grants Scheme |
---|---|
Project Team | Dr Zoë Griffiths, Dr Jennifer Baker, Associate Professor Clovia Holdsworth |
Scheme | Small Grants Scheme |
Role | Investigator |
Funding Start | 2022 |
Funding Finish | 2022 |
GNo | |
Type Of Funding | Internal |
Category | INTE |
UON | N |
HMRI Precision Medicine Research Program Support Scheme$2,164
Funding body: Hunter Medical Research Institute - Precision Medicine Research Program
Funding body | Hunter Medical Research Institute - Precision Medicine Research Program |
---|---|
Project Team | Dr Jennifer Baker |
Scheme | PMRP ECR/MCR Support Scheme |
Role | Lead |
Funding Start | 2022 |
Funding Finish | 2022 |
GNo | |
Type Of Funding | Internal |
Category | INTE |
UON | N |
20213 grants / $343,358
Developing novel agents to prevent tumour recurrence in glioblastoma$312,000
Funding body: NHMRC (National Health & Medical Research Council)
Funding body | NHMRC (National Health & Medical Research Council) |
---|---|
Project Team | Doctor Jennifer Baker, Associate Professor Lenka Munoz, Professor Terrance Johns |
Scheme | Ideas Grants |
Role | Lead |
Funding Start | 2021 |
Funding Finish | 2023 |
GNo | G2100506 |
Type Of Funding | C1100 - Aust Competitive - NHMRC |
Category | 1100 |
UON | Y |
CESE Equipment and Infrastructure Investment Scheme$28,355
Funding body: College of Engineering, Science and Environment, University of Newcastle
Funding body | College of Engineering, Science and Environment, University of Newcastle |
---|---|
Scheme | Equipment and Infrastructure Investment Scheme |
Role | Investigator |
Funding Start | 2021 |
Funding Finish | 2021 |
GNo | |
Type Of Funding | Internal |
Category | INTE |
UON | N |
CESE Lockdown Support Scheme$3,003
Funding body: College of Engineering, Science and Environment, University of Newcastle
Funding body | College of Engineering, Science and Environment, University of Newcastle |
---|---|
Scheme | Lockdown support scheme |
Role | Lead |
Funding Start | 2021 |
Funding Finish | 2021 |
GNo | |
Type Of Funding | Internal |
Category | INTE |
UON | N |
20202 grants / $13,885
Development of Azo-phenylacrylonitriles as selective AhR antagonists$8,885
Funding body: Priority Research Centre for Chemical Biology and Clinical Pharmacology, UoN
Funding body | Priority Research Centre for Chemical Biology and Clinical Pharmacology, UoN |
---|---|
Project Team | Professor Adam McCluskey, Dr Jennette Sakoff |
Scheme | Priority Research Centre for Chemical Biology and Clinical Pharmacology Seed Grant |
Role | Lead |
Funding Start | 2020 |
Funding Finish | 2020 |
GNo | |
Type Of Funding | Internal |
Category | INTE |
UON | N |
Small Equipment Grant$5,000
Funding body: Priority Research Centre for Chemical Biology and Clinical Pharmacology
Funding body | Priority Research Centre for Chemical Biology and Clinical Pharmacology |
---|---|
Scheme | PRC Chemical Biology & Clinical Pharmacology Equipment Grant |
Role | Lead |
Funding Start | 2020 |
Funding Finish | 2020 |
GNo | |
Type Of Funding | Internal |
Category | INTE |
UON | N |
20193 grants / $25,500
Equipment Grant$20,000
Funding body: PRC for Chemical Biology and Pharmacology, The University of Newcastle
Funding body | PRC for Chemical Biology and Pharmacology, The University of Newcastle |
---|---|
Project Team | Jennifer Baker, Adam McCluskey, Cecilia Russell, Nicholas O'Brien, Kate Prichard |
Scheme | Equipment Support Scheme 2019 |
Role | Investigator |
Funding Start | 2019 |
Funding Finish | 2019 |
GNo | |
Type Of Funding | Internal |
Category | INTE |
UON | N |
International Travel Grant$3,500
Funding body: PRC for Chemical Biology and Pharmacology, The University of Newcastle
Funding body | PRC for Chemical Biology and Pharmacology, The University of Newcastle |
---|---|
Project Team | Jennifer Baker |
Scheme | PRC-CBP International Conference Award |
Role | Lead |
Funding Start | 2019 |
Funding Finish | 2019 |
GNo | |
Type Of Funding | Internal |
Category | INTE |
UON | N |
RACI Postgraduate Student Travel Scholarship$2,000
Funding body: Royal Australian Chemical Institute
Funding body | Royal Australian Chemical Institute |
---|---|
Project Team | Jennifer Baker |
Scheme | Postgraduate student travel award |
Role | Lead |
Funding Start | 2019 |
Funding Finish | 2019 |
GNo | |
Type Of Funding | External |
Category | EXTE |
UON | N |
20182 grants / $7,000
Small Equipment Grant$5,000
Funding body: PRC for Chemical Biology and Pharmacology, The University of Newcastle
Funding body | PRC for Chemical Biology and Pharmacology, The University of Newcastle |
---|---|
Project Team | Jennifer Baker, Adam McCluskey |
Scheme | PRC small equipment scheme 2018 |
Role | Lead |
Funding Start | 2018 |
Funding Finish | 2018 |
GNo | |
Type Of Funding | Internal |
Category | INTE |
UON | N |
Higher Degree Research (HDR) Conference Scholarship$2,000
Funding body: Faculty of Science and Information Technology, The University of Newcastle
Funding body | Faculty of Science and Information Technology, The University of Newcastle |
---|---|
Project Team | Jennifer Baker |
Scheme | Higher Degree Research (HDR) Conference Scholarship |
Role | Lead |
Funding Start | 2018 |
Funding Finish | 2018 |
GNo | |
Type Of Funding | Internal |
Category | INTE |
UON | N |
20171 grants / $1,000
Royal Australian Chemical Institute (RACI) Student Bursary$1,000
Funding body: Royal Australian Chemical Institute
Funding body | Royal Australian Chemical Institute |
---|---|
Project Team | Jennifer Baker |
Scheme | Student Bursary for RACI Centenary Congress, 2017 |
Role | Lead |
Funding Start | 2017 |
Funding Finish | 2017 |
GNo | |
Type Of Funding | External |
Category | EXTE |
UON | N |
Research Supervision
Number of supervisions
Current Supervision
Commenced | Level of Study | Research Title | Program | Supervisor Type |
---|---|---|---|---|
2023 | PhD | Design And Synthesis Of Novel Histone Lysine Demethylase Inhibitors | PhD (Chemistry), College of Engineering, Science and Environment, The University of Newcastle | Principal Supervisor |
2020 | PhD | Micro-Dissection of Clathrins Role in Mitosis by Chemical Biology Probes | PhD (Chemistry), College of Engineering, Science and Environment, The University of Newcastle | Co-Supervisor |
Past Supervision
Year | Level of Study | Research Title | Program | Supervisor Type |
---|---|---|---|---|
2022 | Masters | Assessing the Efficacy of Bispidinones as Novel Pancreatic Cancer Therapeutic Agents | M Philosophy (Biological Sc), College of Engineering, Science and Environment, The University of Newcastle | Co-Supervisor |
Research Projects
Targeting Tumour Recurrence in Glioblastoma 2021 -
This project involves utilising molecular modelling methods and structure activity relationships to design new, potent small molecules of a histone lysine demethylase protein for the potential treatment of the deadly brain cancer glioblastoma.
Design and Synthesis of Arylhydrocarbon Receptor Ligands 2016 - 2020
The molecular-modelling led synthesis of small molecules that hijack the Arylhydrocarbon Receptor as potent breast cancer-selective agents.
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Research Collaborations
The map is a representation of a researchers co-authorship with collaborators across the globe. The map displays the number of publications against a country, where there is at least one co-author based in that country. Data is sourced from the University of Newcastle research publication management system (NURO) and may not fully represent the authors complete body of work.
Country | Count of Publications | |
---|---|---|
Australia | 27 | |
United States | 6 | |
China | 4 | |
Viet Nam | 2 | |
Germany | 1 | |
More... |
Dr Jennifer Baker
Positions
Postdoctoral Researcher
School of Environmental and Life Sciences
College of Engineering, Science and Environment
Casual Academic - Open Foundation
Learning and Teaching
Academic Division
Focus area
Chemistry
Contact Details
jennifer.r.baker@newcastle.edu.au | |
Link | Research Networks |
Office
Room | C216c. |
---|---|
Building | Chemistry Building |
Location | Callaghan University Drive Callaghan, NSW 2308 Australia |