2 research outputs found
Synthesis of Sulfur-Containing Heterocycles through Oxidative Carbon–Hydrogen Bond Functionalization
Vinyl sulfides react rapidly and efficiently with 2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ) to form α,β-unsaturated thiocarbenium ions through oxidative carbon–hydrogen bond cleavage. These electrophiles couple with appended π-nucleophiles to yield sulfur-containing heterocycles through carbon–carbon bond formation. Several nucleophiles are compatible with the procedure, and the reactions generally proceed through readily predictable transition states
Synthesis and Biological Evaluation of Neopeltolide and Analogs
The synthesis of neopeltolide analogues that contain
variations in the oxazole-containing side chain and in the macrolide
core are reported along with the GI<sub>50</sub> values for these
compounds against MCF-7, HCT-116, and p53 knockout HCT-116 cell lines.
Although biological activity is sensitive to changes in the macrocycle
and the side chain, several analogues displayed GI<sub>50</sub> values
of <25 nM. Neopeltolide and several of the more potent analogues
were significantly less potent against p53 knockout cells, suggesting
that p53 plays an auxiliary role in the activity of these compounds