https://nova.newcastle.edu.au/vital/access/ /manager/Index en-au 5 https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:12632 Wed 11 Apr 2018 13:22:57 AEST ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:34760 BisP1: 1,5-diphenyl-3,7-bis(2-hydroxyethyl)-3,7-diazabicyclo[3.3.1]nonan-9-one; BisP2: 3,7-bis-(2-(S)-amino-4-methylsulfanylbutyryl)-1,5-diphenyl-3,7-diazabicyclo[3.3.1]nonan-9-one dihydrochloride; BisP3: [2-{7-[2-(S)-tert-butoxycarbonylamino-3-(1H-indol-3-yl)-propionyl]-9-oxo-1,5-diphenyl-3,7-diazabicyclo[3.3.1]non-3-yl}-1-(S)-(1H-indol-3-ylmethyl)-2-oxoethyl]-carbamic acid tertbutyl ester; BisP4: 3,7-bis-[2-(S)-amino-3-(1H-indol-3-yl)-propionyl]-1,5-diphenyl-3,7-diazabicyclo[3.3.1]nonan-9-one dihydrochloride) was assessed against PC cell lines (MiaPaca-2, CFPAC-1 and BxPC-3). Cell viability was assessed using a Cell Counting Kit-8 (CCK-8) colorimetric assay, while apoptotic cell death was confirmed using fluorescence microscopy and flow cytometry. Initial viability screening revealed significant cytotoxic activity from BisP4 treatment (1 µM⁻100 µM) on all three cell lines, with IC50 values for MiaPaca-2, BxPC-3, and CFPAC-1 16.9 µM, 23.7 µM, and 36.3 µM, respectively. Cytotoxic treatment time-response (4 h, 24 h, and 48 h) revealed a 24 h treatment time was sufficient to produce a cytotoxic effect on all cell lines. Light microscopy evaluation (DAPI staining) of BisP4 treated MiaPaca-2 PC cells revealed dose-dependent characteristic apoptotic morphological changes. In addition, flow cytometry confirmed BisP4 induced apoptotic cell death induction of activated caspase-3/-7. The bispidinone derivative BisP4 induced an apoptosis-mediated cytotoxic effect on MiaPaca-2 cell lines and significant cytotoxicity on CFPAC-1 and BxPC-3 cell lines. Further investigations into the precise cellular mechanisms of action of this class of compounds are necessary for potential development into pre-clinical trials.]]> Thu 17 Mar 2022 14:34:42 AEDT ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:44082 in vitro and orthotopic tumour growth in vivo. Dynamin inhibition reduced glioblastoma cell line viability and suppressed neurosphere formation and migration of GSCs. Tumour growth was reduced by CyDyn 4-36 treatment. Dynamin 2 inhibition therefore represents a novel approach for stem cell-directed Glioblastoma therapy.]]> Thu 06 Oct 2022 15:06:34 AEDT ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:12397 50s of 25–40 μM. The high ‘hit rate’ (5.6%) indicates that the approach taken here has advantages over conventional drug screening methods. A major advantage of norcantharidin analogues over some other currently available anthelmintics is that they can be produced in one to two steps in large amounts at low cost and high purity, and do not require any additional steps for the isolation of the active isomer. This positions them well for commercial development.]]> Sat 24 Mar 2018 08:15:45 AEDT ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:17426 Sat 24 Mar 2018 08:01:40 AEDT ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:19942 Sat 24 Mar 2018 07:58:35 AEDT ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:17938 Sat 24 Mar 2018 07:56:33 AEDT ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:17940 Sat 24 Mar 2018 07:56:29 AEDT ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:20974 Sat 24 Mar 2018 07:54:19 AEDT ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:22223 100 μM), as per the parent molecule. We also discovered that the introduction of a terminal phosphate moiety (28) at the same position produced a different trend in cytotoxicity with strong activity in BE2-C (neuroblastoma; GI₅₀ = 9 μM) cells; suggestive of an alternate mode of action.]]> Sat 24 Mar 2018 07:17:43 AEDT ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:22284 Sat 24 Mar 2018 07:17:40 AEDT ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:22226 Sat 24 Mar 2018 07:17:37 AEDT ]]> https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:42808 Mon 05 Sep 2022 09:57:19 AEST ]]>