52273-78-6Relevant articles and documents
Optical Control of Mitosis with a Photoswitchable Eg5 Inhibitor
Impastato, Anna C.,Shemet, Andrej,Vep?ek, Nynke A.,Saper, Gadiel,Hess, Henry,Rao, Lu,Gennerich, Arne,Trauner, Dirk
, (2022/01/20)
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.
HALOETHYL UREA COMPOUNDS AND THEIR USE TO ATTENUATE, INHIBIT OR PREVENT NON-CANCEROUS PATHOGENIC CELLULAR PROLIFERATION AND DISEASES ASSOCIATED THEREWITH
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Page 78-79, (2010/02/09)
The present invention provides haloethyl urea compounds as described in Formula (I) and their use as anti-proliferative agent in the attenuation, inhibition, or prevention of non-cancerous cellular proliferation. These compounds are also provided for use as a therapeutic agent in the treatment of a disease or disorder, wherein pathogenesis of said disease or disorder is associated with non-cancerous pathogenic cellular proliferation.
CYCLOPENTENE DERIVATIVES USEFUL AS ANTAGONISTS OF THE MOTILIN RECEPTOR
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Page 24, (2010/02/06)
The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor disorders. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.