https://nova.newcastle.edu.au/vital/access/ /manager/Index ${session.getAttribute("locale")} 5 https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:44078 6] and the protic ionic liquid ethanolammonium nitrate (ETAN) failed. Microwave irradiation in EAN facilitated rapid access to three focused libraries, based on the parent isocyanide: cyclohexyl isocyanide, benzyl isocyanide and ethyl isocyanoacetate. Analysis of the structure activity relationship data suggested the presence of a bulky moiety originating from the isocyanide (cyclohexyl and benzyl) enhanced cytotoxicity. Removal of the acetylenic H-atom from the ethanoic acid moiety was detrimental to cytotoxicity. The most active analogues produced, N-(2-cyclohexylamino)-1-(4-methoxyphenyl)-2-oxoethyl-N-(3,5-dimethoxyphenyl)propiolamide, returned average GI₅₀ values of ≤1 μM across the cancer cell lines evaluated. Combined, these data suggest that analogues of this nature are interesting potential anti-cancer development leads.]]> Wed 26 Oct 2022 10:31:27 AEDT ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:34053 Wed 04 Sep 2019 09:39:49 AEST ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:20160 36-fold reduced activity against rings, suggesting that they can discriminate between helical or ring oligomerization states. 4a and 6a inhibited dynamin-dependent endocytosis of transferrin in multiple cell types (IC50 of 5.7 and 5.8 μM, respectively), at least sixfold more potently than dynasore, but had no effect on dynamin-independent endocytosis of cholera toxin. 4a also reduced synaptic vesicle endocytosis and activity-dependent bulk endocytosis in cultured neurons and synaptosomes. Overall, 4a and 6a are improved and versatile helical dynamin and endocytosis inhibitors in terms of potency, non-specific binding and cytotoxicity. The data further suggest that the ring oligomerization state of dynamin is not required for clathrin-mediated endocytosis.]]> Tue 24 Aug 2021 14:23:34 AEST ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:54007 Thu 25 Jan 2024 13:53:31 AEDT ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:32119 (CME) = 65.9 ± 7.7 to 3.7 ± 1.1 mM), which makes this series among the more potent inhibitors of dynamin and CME yet reported. In CME and growth inhibition cell-based assays, the data obtained was consistent with dynamin inhibition. CEREP ExpresS profiling identified off-target effects at the cholecystokinin, dopamine D₂, histamine H₁ and H₂, melanocortin, melatonin, muscarinic M₁ and M₃, neurokinin, opioid KOP and serotonin receptors.]]> Thu 03 May 2018 12:18:53 AEST ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:19893 Sat 24 Mar 2018 07:57:02 AEDT ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:19892 Sat 24 Mar 2018 07:57:02 AEDT ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:20625 Sat 24 Mar 2018 07:55:46 AEDT ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:21262 Sat 24 Mar 2018 07:54:43 AEDT ]]>