3524-69-4Relevant academic research and scientific papers
Benzofuran derivatives as anticancer inhibitors of mTOR signaling
Salomé, Christophe,Ribeiro, Nigel,Chavagnan, Thierry,Thuaud, Frédéric,Serova, Maria,De Gramont, Armand,Faivre, Sandrine,Raymond, Eric,Désaubry, Laurent
supporting information, p. 181 - 191 (2014/06/09)
A series of 32 derivatives and isosteres of the mTOR inhibitor 2 were synthesized and compared for their cytotoxicity in radioresistant SQ20B cancer cell line. Several of these compounds, in particular 30b, were significantly more cytotoxic than 2. Importantly, 30b was shown to block both mTORC1 and Akt signaling, suggesting insensitivity to the resistance associated to Akt overactivation observed with rapamycin derivatives currently used in clinic.
New chemical tools for investigating human mitotic kinesin Eg5
Klein, Emmanuel,DeBonis, Salvatore,Thiede, Bernd,Skoufias, Dimitrios A.,Kozielski, Frank,Lebeau, Luc
, p. 6474 - 6488 (2008/09/17)
We have designed and synthesized a series of monastrol derivatives, an allosteric inhibitor of Eg5, a motor protein responsible for the formation and maintenance of the bipolar spindle in mitotic cells. Sterically demanding structural modifications have been introduced on the skeleton of the parent drug either via a multicomponent Biginelli reaction or a stepwise modification of monastrol. The ability of these compounds to inhibit Eg5 activity has been investigated using two in vitro steady-state ATPase assays (basal and microtubule-stimulated) as well as a cell-based assay. One compound in the series appeared more potent than monastrol by a fivefold factor. Three other compounds that were unable to inhibit Eg5 ATPase activity in vitro proved potent Eg5 inhibitors in the cell-based assay. The results obtained led to the identification of structure-activity relationships further used to design an affinity matrix that can be used for fast and efficient purification of Eg5 from crude lysate of eukaryotic cells.
Novel compounds useful for modulating abnormal cell proliferation
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Page/Page column 8, (2008/06/13)
There is described compounds of Formulae I, II, III, IV and V. The compounds of Formulae I, II, III, IV and/or V are useful: in therapeutic methods and compositions for modulating cell proliferation, in diagnostic assays and as research tools.
Convenient synthesis of a simple coumarin from salicylaldehyde and wittig reagent. IV: Improved synthetic method of substituted coumarins
Takeuchi, Yasuo,Ueda, Norihiro,Uesugi, Koji,Abe, Hitoshi,Nishioka, Hiromi,Harayama, Takashi
, p. 217 - 224 (2007/10/03)
The reaction of salicylaldehydes (2) with Horner-Wadsworth-Emmons (HWE) or Ando-HWE reagents was attempted to afford intramolecular phosphonate derivatives (6). A new synthetic method for coumarins (1) was achieved by using protected 2.
