/manager/Index ${session.getAttribute("locale")} 5 Synthesis, molecular modeling and biological activity of methyl and thiomethyl substituted pyrimidines as corticotropin releasing hormone type 1 antagonists /manager/Repository/uon:1663 50 : 1 noted. All analogues were screened for their ability to interact with CRH₁ and CRH₂ receptors. In all instances only poor agonistic and/or antagonistic behaviour was noted at CRH₂. However, several compounds were potent and selective CRH₁ antagonists, most notably 13a Ki = 39nM. Additionally we have utilized these data and that recently reported by others to refine our original CRH₁ pharmacophore.]]> Sat 24 Mar 2018 08:30:27 AEDT ]]> Cantharidin analogues: synthesis and evaluation of growth inhibition in a panel of selected tumour cell lines /manager/Repository/uon:1773 1000 μM. Analogues possessing good PP1 and/or PP2A inhibition also returned moderate to good anti-cancer activity. Analogues with substituents directly attached to the intact bicyclo[2.2.1]heptane skeleton were poor to moderate anti-cancer agents. This correlates well with their lack of PP1 or PP2A activity. Analogues capable of undergoing a facile ring opening of the anhydride or with a single carboxylate were good PP1 and PP2A inhibitors, largely correlating to the observed anti-cancer activity in all cases, except 11. Analogue 11, whist neither a PP1 nor a PP2A inhibitor shows anti-cancer activity comparable to 1 and 2. We believe that intracellular esterases generate the corresponding dicarboxylate, which is a potent PP1 and PP2A inhibitor, and that it is this species which is responsible for the observed anti-cancer activity.]]> Sat 24 Mar 2018 08:27:36 AEDT ]]> Combining structure-based drug design and pharmacophores /manager/Repository/uon:295 Sat 24 Mar 2018 07:43:42 AEDT ]]> BiCl3-mediated opening of epoxides, a facile route to chlorohydrins or amino alcohols: one reagent, two paths /manager/Repository/uon:341 Sat 24 Mar 2018 07:42:27 AEDT ]]> Identification of aminopyrimidine regioisomers via line broadening effects in ¹H and ¹³C NMR spectroscopy /manager/Repository/uon:3267 Sat 24 Mar 2018 07:21:22 AEDT ]]>