https://ogma.newcastle.edu.au/vital/access/ /manager/Index en-au 5 https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:29353 70/σ^A interaction as determined by ELISA and exhibiting increased inhibition of the growth of Escherichia coli compared to Bacillus subtilis in culture. The structural features of the synthesized transcription initiation inhibitors needed for antibacterial activity were identified employing molecular modelling and structure–activity relationship (SAR) studies.]]> Wed 15 Dec 2021 16:09:32 AEDT ]]> https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:18018 Wed 11 Apr 2018 15:54:12 AEST ]]> https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:10405 Sat 24 Mar 2018 08:07:46 AEDT ]]> https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:17424 Sat 24 Mar 2018 08:01:39 AEDT ]]> https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:19942 Sat 24 Mar 2018 07:58:35 AEDT ]]> https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:20965 Sat 24 Mar 2018 07:54:22 AEDT ]]> https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:18787 50) of 42 μM in MCF-7 (breast) cells and 24 μM in A2780 (ovarian) cells and >50 μM in all other cell lines tested. The development of eight focused libraries comprising thirty compounds total identified N-(biphenyl-4-ylmethyl)-1H-pyrrole-2-carboxamide (4l), N-benzyl-4,5-dibromo-1H-pyrrole-2-carboxamide (5a) and N-(biphenyl-4-ylmethyl)-4,5-dibromo-1H-pyrrole-2-carboxamide (5l) as potent inhibitors of cell growth in our panel of cell lines. Of these compounds GI₅₀ values of <5 μM were observed with 4l against HT29 (colon) and SW480 (colon); 5a against HT29; and 5l against HT29, SW480, MCF-7, A431 (skin), Du145 (prostate), BE2-C (neuroblastoma) and MIA (pancreas) cell lines. As a cancer class, colon cancer appears to be more sensitive to the oroidin series of compounds, with analogue 5l being the most active.]]> Sat 24 Mar 2018 07:51:02 AEDT ]]> https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:27697 70/σ^A factors in bacteria. In this study, the reaction of indole-2-, indole-3-, indole-7- and benzofuran-2-glyoxyloyl chlorides with amines and hydrazines afforded a variety of glyoxyloylamides and glyoxyloylhydrazides. Similarly, condensation of 2- and 7-trichloroacetylindoles with amines and hydrazines delivered amides and hydrazides. The novel molecules were found to inhibit the RNA polymerase-σ⁷⁰/σ^A interaction as measured by ELISA, and also inhibited the growth of both Gram-positive and Gram-negative bacteria in culture. Structure-activity relationship (SAR) studies of the mono-indole and mono-benzofuran inhibitors suggested that the hydrophilic-hydrophobic balance is an important determinant of biological activity.]]> Sat 24 Mar 2018 07:40:09 AEDT ]]> https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:28988 a]pyrazine derivatives has been developed as inhibitors of the VirB11 ATPase HP0525, a key component of the bacterial type IV secretion system. A flexible synthetic route to both 2- and 3-aryl substituted regioisomers has been developed. The resulting series of imidazo[1,2-a]pyrazines has been used to probe the structure-activity relationships of these inhibitors, which show potential as antibacterial agents.]]> Sat 24 Mar 2018 07:29:24 AEDT ]]> https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:28318 50), respectively. Of note, were a CF₃ functionalised anthracenone 4-pyranone (chromone) derivative 22, and an anthracenone-furan derivative 54 which displayed 0.20µM and 0.38µM growth inhibition, respectively, in the BE2-C neuroblastoma cell line.]]> Sat 24 Mar 2018 07:25:08 AEDT ]]> https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:3263 Sat 24 Mar 2018 07:21:22 AEDT ]]> https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:3264 Sat 24 Mar 2018 07:21:22 AEDT ]]> https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:3428 Sat 24 Mar 2018 07:20:26 AEDT ]]>