A library of epothilone A and B analogues, which was constructed by solid-phase combinatorial synthesis using SMART Microreactors and solution chemistry, was screened in two different tubulin binding assays. Selected compounds were subjected to cytotoxicity studies against a number of cell lines, including Taxol-resistant cells. Important structure–activity relationship emerged from these studies, which sets the stage for further discoveries and developments in the anticancer field
A combination of rolling circle amplification and nicking endonuclease-assisted nanoparticle amplification (NEANA) is used for the rapid, colorimetric detection of DNA. The integration of rolling circle amplification into the NEANA approach allows for detection of oligonucleotides with arbitrary sequences at ultralow concentrations.
COMMUNICATIONS component 7 to give 24, and with subsequent cycloreversion to the conjugated diene 8. The fact that coupling is limited to terminal alkynes may have a steric origin. Formation of the more stable and thus less reactive conjugated carbene complex 23 might explain why the yne-ene metathesis requires longer reaction times than conventional cross-metathesis between alkenes. Volatile ethylene is formed in the cross-metathesis of terminal alkenes, whereas the yne-ene metathesis takes place with atom economy. The driving force in yne-ene metathesis may be the formation of a conjugated diene.The type of reaction described here is, to our knowledge, the first selective crossed yne-ene metathesis. Application of this cross-metathesis between terminal alkynes and alkenes has been demonstrated by the synthesis of variously functionalized dienes. The reaction opens the way to interesting structural elements: thus, conjugated allylsilanes have found a variety of applications, for example in Sakurai reactions.['*] The metathesis products are also of interest with respect to Diels-Alder reactions and cycloadditions. We are currently investigating the applications of yne-ene metathesis in natural product synthesis.
Flap structure-specific
endonuclease 1 (FEN1) is overexpressed
in various types of human cancer cells and has been recognized as
a promising biomarker for cancer diagnosis in the recent years. In
order to specifically detect the abundance and activity of this cancer-overexpressed
enzyme, different types of DNA-based nanodevices were created during
our investigations. It is shown in our studies that these newly designed
biosensors are highly sensitive and specific for FEN1 in living cells
as well as in cell-free systems. It is expected that these nanoprobes
could be useful for monitoring FEN1 activity in human cancer cells,
and also for cell-based screening of FEN1 inhibitors as new anticancer
drugs.
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