- Optical Control of Mitosis with a Photoswitchable Eg5 Inhibitor
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Eg5 is a kinesin motor protein that is responsible for bipolar spindle formation and plays a crucial role during mitosis. Loss of Eg5 function leads to the formation of monopolar spindles, followed by mitotic arrest, and subsequent cell death. Several cell-permeable small molecules have been reported to inhibit Eg5 and some have been evaluated as anticancer agents. We now describe the design, synthesis, and biological evaluation of photoswitchable variants with five different pharmacophores. Our lead compound Azo-EMD is a cell permeable azobenzene that inhibits Eg5 more potently in its light-induced cis form. This activity decreased the velocity of Eg5 in single-molecule assays, promoted formation of monopolar spindles, and led to mitotic arrest in a light dependent way.
- Impastato, Anna C.,Shemet, Andrej,Vep?ek, Nynke A.,Saper, Gadiel,Hess, Henry,Rao, Lu,Gennerich, Arne,Trauner, Dirk
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- PROCESS FOR PREPARING TETRAHYDROQUINOLINE DERIVATIVES
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The invention relates to a novel process for preparing enantiomerically enriched or pure tetrahydroquinoline derivatives by reacting a chiral dihydropyran-methylamine C with a aldehyde B and an aniline A in a multicomponent one pot synthesis in the presen
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Page/Page column 34-36
(2009/07/18)
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- POLYMORPHIC FORMS AND PROCESS
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The invention relates to a process for the manufacture of enantiomerically enriched or pure compounds of formula (I) wherein R1, R2, R3, R6, R7 and Q are defined as in claim 1 as well as their crystal
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Page/Page column 30
(2008/06/13)
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