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In the present research, we designed several ATRA derivatives having a hydrophobic alkyl ketone moiety instead of the negatively charged carboxylic acid moiety.
It can be concluded that the ifenprodil binding site of GluN2B subunit containing NMDA receptors well tolerates a vinyl or hydroxymethyl moiety instead of the benzylic OH group.
Preliminary biological evaluation of the analogues using the bovine thymus vitamin D receptor (VDR) suggested that the incorporation of the spiro-oxetane moiety instead of a gem-dimethyl group at the C2 position had a beneficial effect on the VDR affinity.
Thus, incorporation of a piperazine moiety instead of an inert alkanedioxy linker alone significantly enhances the DNA binding ability, and the analogous dimer 4 that lacks a piperazine moiety in the linker spacer elevates melting by only 15.1 °C under identical experimental conditions.
Comparison of its NMR spectroscopic data (Tables 1, 2) with those of 1 revealed they are structural analogues with the obvious difference being the presence of an α,β-unsaturated-γ-lactone moiety instead of the β-substituted furan ring.
These new salts were retested in the same in vitro assays and were confirmed to have the same phenotypes as seen for pyrvinium pamoate, verifying that the pyrvinium moiety, instead of pamoate, is responsible for the observed phenotypes since pamoate alone did not show any observable effect (Figure S2).
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Some of the 2-PQs studied had a two ring-moiety instead of the phenyl group as a C-ring.
Reactions 19-22 correspond to reactions 14-17, except for the fact that in this case P C N Aon carries two linked ubiquitin moieties instead of a single one.
As part of our studies to change the DNA binding mode of triostin A and its derivatives from bisintercalation to specific major groove recognition, the rigid templating depsipeptide scaffold is used to organize nucleobases or other recognition moieties instead of the native quinoxaline moieties (Lorenz and Diederichsen 2004).
26 As already mentioned above, an alternative reaction pathway has been identified for the ODH-process of the [V2P2O10].+ cluster in which a structural isomer of 10, that is, 10 – 2 in Figure 3, is generated bearing two P OH moieties instead of the P OH/V OH groups as in 10.
Compound 13 bears the nicotinamide moiety of nicorandil instead of nitrate ester.
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