1076-47-7Relevant articles and documents
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Reichstein et al.
, p. 412,415 (1936)
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Isosteric analogs of lenalidomide and pomalidomide: Synthesis and biological activity
Ruchelman, Alexander L.,Man, Hon-Wah,Zhang, Weihong,Chen, Roger,Capone, Lori,Kang, Jian,Parton, Anastasia,Corral, Laura,Schafer, Peter H.,Babusis, Darius,Moghaddam, Mehran F.,Tang, Yang,Shirley, Michael A.,Muller, George W.
, p. 360 - 365 (2013/02/23)
A series of analogs of the immunomodulary drugs lenalidomide (1) and pomalidomide (2), in which the amino group is replaced with various isosteres, was prepared and assayed for immunomodulatory activity and activity against cancer cell lines. The 4-methyl and 4-chloro analogs 4 and 15, respectively, displayed potent inhibition of tumor necrosis factor-α (TNF-α) in LPS-stimulated hPBMC, potent stimulation of IL-2 in a human T cell co-stimulation assay, and anti-proliferative activity against the Namalwa lymphoma cell line. Both of these analogs displayed oral bioavailability in rat.
Hydrocarbures arylaliphatiques. Partie VIII. Etude cinetique de la protodesilylation de benzocyclenes tricycliques
Gruber, Rene,Kirsch, Gilbert,Cagniant, Denise
, p. 498 - 504 (2007/10/02)
A kinetic study of the protodesilylation of silylated derivatives of hemimellitene, 2a,3,4,5 tetrahydro acenaphthene and 1H 2,2a,3,4,5,6 hexahydro benzo(c,d)azulene is described.These results complete those published previously and which are related to the influence of the ring size of alicyclic systems pericondensed to a benzene nucleus on the reactivity of the nucleus to acetylation or bromination.The silylated derivatives were prepared from the corresponding bromo compounds.The synthesis of the bromo compounds, some of which were described in an earlier study, is completed here by using a synthetic pathway which allows the preparation of the β isomers starting from the ortho bromo derivatives.The kinetic results show a deactivation of the β position of the hemimellitene.A little deactivation of ortho α position of the five membered ring in the tricyclic compounds is also observed.This last result, significant in the case of bromination, seems to be related to the Mills-Nixon effect and can be explained by using Streitwieser's hybridization for the ? skeleton.