PubMed · 14755261
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Eric J Amis. 2004. Reaching beyond discovery.. https://doi.org/10.1038/nmat1064
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The SAR of the lead compounds 2a and 2b was rapidly explored. Utilizing a parallel solution-phase Suzuki coupling approach, in tandem with strong cation exchange resin (SCX) purification afforded the desired focused library. The library was evaluated in vitro, a ninefold potency increase was achieved and the preference for ortho substitution of moderate steric bulk of the fourth, phenyl ring was identified. In addition, dimethylisoxazole, as a heterocyclic replacement for the phenylic ring of the lead compound, was also identified by this approach.
We report the discovery of a new class of light-sensing molecules. These light sensors are composed of fluorophore oligomers assembled on a DNA backbone. A combinatorial library of tetrafluorophores consisting of over 14 000 compounds was synthesized and screened for rapid responses toward light exposure. Among the most light-sensitive molecules, at least three tetramers were found to respond to light exposure with apparent color changes, rather than simple photobleaching.
[structure: see text] A new type of glycocluster based on polyhedral oligosilsesquioxanes (POSS) has been efficiently prepared from unprotected mannoside and lactoside employing a convergent approach of thiol-radical addition reaction. The versatility of this approach was demonstrated by functionalization of mannosides and lactosides of different-length spacers.