https://nova.newcastle.edu.au/vital/access/ /manager/Index en-au 5 A methanol and protic ionic liquid Ugi multicomponent reaction path to cytotoxic a-phenylacetamido amides 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 ]]> Development of novel PP2A activators for use in the treatment of acute myeloid leukaemia https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:29815 Wed 24 Nov 2021 15:50:53 AEDT ]]> The membrane protein sortilin can be targeted to inhibit pancreatic cancer cell invasion https://nova.newcastle.edu.au/vital/access/ /manager/Repository/uon:37858 P = 0.0014). Sortilin inhibition by siRNA and the pharmacologic inhibitor AF38469 strongly reduced the adhesion and invasion of pancreatic cancer cells without affecting cell survival and viability. Sortilin inhibition also decreased the phosphorylation of the focal adhesion kinase in Tyr925. Together, these data show that sortilin contributes to pancreatic cancer invasion and could eventually be targeted in therapy.]]> Thu 24 Mar 2022 11:34:45 AEDT ]]>