129044-99-1Relevant academic research and scientific papers
Compounds interacting with tubulin. Part II fll : Synthesis of tricyclic lactams with a phenylpyrrole framework, structural analogs of rhazinilam
Alazard, Jean-Pierre,Millet-Paillusson, Corinne,Guenard, Daniel,Thai, Claude
, p. 251 - 266 (2007/10/03)
The biolooical interest of rhazinilam 1 led us to synthesize the tricydic lactam analogs 4-9 with different alkyl substituents in the a and β positions on the pyrrole ring, and different sizes of the lactam ring (6-, 7-, 8- and 9-membered). These compounds were prepared from arylpyrrole 12 (access to lactams 4-8) and arylpyrrole 49 (access to lactam 9). The in vitro biological activities of all these analogs (evaluated by an antitubulin test) were found to be inferior to that of rhazinilam 1, but were nevertheless of the same type. The results are discussed. Elsevier,.
Compounds interacting with tubulin: Part I: Synthesis of ortho-ortho' substituted phenylpyrroles with free or restricted rotation.
Alazard, JP.,Boye, O.,Gillet, B.,Guenard, D.,Beloeil, JC.,Thal, C.
, p. 779 - 787 (2007/10/02)
The synthesis of ortho-ortho' substituted phenylpyrroles that are susceptible to isomerization of the biaryl type (atropisomerism) was performed using a Michael addition of isocyanoacetates with nitrostyrenes.Atropisomerism in phenylpyrroles 14 and 15 was studied by means of 1H NMR spectroscopy using chiral lanthanide shift reagents (LSR*).In the case of chiral phenylpyrrole 21, an evaluation of the interconversion parameters between diastereomers (k, ΔGT*) was attempted. - - - tubulin / phenylpyrrole / atropisomers / chiral shift reagents
Phenylpyrrolic compounds used as drugs, their preparation and application
-
, (2008/06/13)
The present invention relates to phenylpyrrole compounds, pharmaceutical compositions, preparation and to their application as an active principle, especially as a drug having antimitotic activity.
