https://nova.newcastle.edu.au/vital/access/ /manager/Index en-au 5 The expanding utility of continuous flow hydrogenation https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:28469 Wed 11 Apr 2018 10:47:35 AEST ]]> Targeting the S100A2-p53 Interaction with a Series of 3,5-Bis(trifluoromethyl)benzene Sulfonamides: Synthesis and Cytotoxicity https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:48769 Wed 05 Apr 2023 14:02:39 AEST ]]> Cytotoxic 1,2,3-Triazoles as Potential Leads Targeting the S100A2-p53 Complex: Synthesis and Cytotoxicity https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:48768 Wed 05 Apr 2023 13:55:29 AEST ]]> Small-molecule inhibitors of the NusB-NusE protein-protein interaction with antibiotic activity https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:34052 Escherichia coli and Gram-positive Bacillus subtilis species, these analogues showed up to 100% growth inhibition at 200 μM. 2-((Z)-4-(((Z)-4-(4-((E)-(Carbamimidoylimino)methyl)phenoxy)but-2-en-1-yl)oxy)benzylidene)hydrazine-1-carboximidamide 22 showed excellent activity against important pathogens. With minimum inhibitory concentration values of ≤3 μg/mL for Gram-positive Streptococcus pneumoniae and methicillin-resistant Staphylococcus aureus and ≤51 μg/mL for Gram-negative Pseudomonas aeruginosa and Acinetobacter baumannii, 22 is a potent lead for a novel antibacterial target. Epifluorescence studies in live bacteria were consistent with 22, inhibiting the NusB–NusE PPI as proposed.]]> Wed 04 Sep 2019 09:54:32 AEST ]]> Novel piperazine-1,2,3-triazole leads for the potential treatment of pancreatic cancer https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:54455 Tue 27 Feb 2024 13:53:27 AEDT ]]> Crystal Structure of Ethyl 2,4-Dimethyl-1-phenyl-6-thioxo-1,6-dihydropyrimidine-5-carboxylate: The Product from the Reaction of Ethyl 3-Aminocrotonate, Phenylisothiocyanate and Acetic Anhydride https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:43145 Tue 13 Sep 2022 15:21:31 AEST ]]> Wiskostatin and other carbazole scaffolds as off target inhibitors of dynamin I GTPase activity and endocytosis https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:50247 Tue 11 Jul 2023 14:16:11 AEST ]]> Amino Alcohols as Potential Antibiotic and Antifungal Leads https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:51456 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) showing >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-dichlorophenyl)-3-(4-(2-hydroxy-3-(D-11-piperidin-1-yl)propoxy)phenyl)-acrylonitrile, and (Z)-3-(4-(3-(4-cyclohexylpiperazin-1-yl)-2-hydroxypropoxy)-phenyl)-2-(3,4-dichlorophenyl)-acrylonitrile 32 μg/mL against Staphylococcus aureus.]]> Tue 05 Sep 2023 18:22:02 AEST ]]> 3,5-Bis(trifluoromethyl)phenylsulfonamides, a novel pancreatic cancer active lead. Investigation of the terminal aromatic moiety https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:48035 47 (3-Cl) > 46 (2-Cl)) against the cell lines examined. The introduction of bulky aromatic moieties was well tolerated, e.g. dihydrobenzo[b][1,4]dioxine (51) returned cohort-2 GI50 values of 1.2-3.4 μM. In all instances the observed docked binding poses and binding scores were consistent with the observed cytotoxicity. This in turn supports, but does not prove, that these analogues function via S100A2-p53 binding groove inhibition.]]> Thu 16 Feb 2023 11:04:01 AEDT ]]> Expanding the utility of flow hydrogenation - a robust protocol restricting hydrodehalogenation https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:19846 Sat 24 Mar 2018 07:57:06 AEDT ]]> Identification and validation of small molecule modulators of the NusB-NusE interaction https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:27293 Bacillus subtilis and Gram-negative Escherichia coli growth.]]> Sat 24 Mar 2018 07:40:19 AEDT ]]> Protein-protein interactions as antibiotic targets: a medicinal chemistry perspective https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:46213 Mon 14 Nov 2022 11:58:08 AEDT ]]> In situ epoxide generation by dimethyldioxirane oxidation and the use of epichlorohydrin in the flow synthesis of a library of beta-amino alcohols https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:36503 3 catalysed microwave ring opening with amines afforded a select range of β-amino alcohols, but with lower levels of aminolysis regiocontrol than the sequential flow approach.]]> Fri 22 May 2020 16:51:41 AEST ]]>