51079-10-8Relevant articles and documents
Photoactivatable caged prodrugs of VEGFR-2 kinase inhibitors
Pinchuk, Boris,Horbert, Rebecca,D?bber, Alexander,Kuhl, Lydia,Peifer, Christian
, (2016)
In this study, we report on the design, synthesis, photokinetic properties and in vitro evaluation of photoactivatable caged prodrugs for the receptor tyrosine kinase VEGFR-2. Highly potent VEGFR-2 inhibitors 1 and 3 were caged by introduction of a photoremovable protecting group (PPG) to yield the caged prodrugs 4 and 5. As expected, enzymatic and cellular proliferation assays showed dramatically diminished efficacy of caged prodrugs in vitro. Upon ultraviolet (UV) irradiation of the prodrugs original inhibitory activity was completely restored and even distinctly reinforced, as was the case for the prodrug 4. The presented results are a further evidence for caging technique being an interesting approach in the protein kinase field. It could enable spatial and temporal control for the inhibition of VEGFR-2. The described photoactivatable prodrugs might be highly useful as biological probes for studying the VEGFR-2 signal transduction.
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Nogrady,Doyle
, p. 485 (1964)
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Synthesis and anti-tumor activity of marine alkaloids
Chen, Guangying,Huang, Gangliang,Zhou, Shiyang
, (2021/04/15)
Marine alkaloids were divided into five categories from the perspective of anti-tumor activity. The optimization process, chemical synthesis, anti-tumor activity evaluation and structure–activity relationship of various compounds were discussed.
Copper-catalyzed carbonylative transformations of indoles with hexaketocyclohexane
Wang, Zechao,Yin, Zhiping,Wu, Xiao-Feng
supporting information, p. 4798 - 4801 (2018/05/23)
With hexaketocyclohexane octahydrate as the carbon monoxide source, a novel procedure for copper-catalyzed direct double carbonylation of indoles has been established. Using alcohols as reaction partners, moderate to good yields of the desired double carbonylation products have been obtained. Wide functional group tolerance and substrate scope can be observed.
Enantioselective Model Synthesis and Progress toward the Putative Structure of Yuremamine
Ghosh, Avipsa,Bainbridge, David T.,Stanley, Levi M.
, p. 7945 - 7951 (2016/09/12)
An enantioselective model synthesis of the 2,3-dihydro-1H-pyrrolo[1,2-a]indole core of the putative structure of yuremamine is reported in 39% overall yield and 96% ee over five steps. The model synthesis leverages enantioselective, rhodium-catalyzed hydroacylation of an N-vinylindole-2-carboxaldehyde as the key step in the installation of the stereochemical triad. An enantioselective synthesis of a densely functionalized dihydropyrroloindolone that maps onto the putative structure of yuremamine is demonstrated in 26% yield and 97% ee over eight steps.
