https://ogma.newcastle.edu.au/vital/access/ /manager/Index en-au 5 https://ogma.newcastle.edu.au/vital/access/ /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 ]]> https://ogma.newcastle.edu.au/vital/access/ /manager/Repository/uon:3324 40- and >30-fold selectivity) over PP2A. Both compounds exhibited moderate PP1 activity, 3 IC₅₀ 50 μM and 6 IC₅₀ 12.5 μM. Interestingly, the corresponding mono-ester derivatives of 3 showed no such selectivity.]]> Sat 24 Mar 2018 07:23:20 AEDT ]]>