685103-48-4Relevant academic research and scientific papers
Synthesis and biological activity of pyrrole analogues of combretastatin A-4
Jung, Eun-Kyung,Leung, Euphemia,Barker, David
, p. 3001 - 3005 (2016)
A series of pyrrole analogues of combretastatin (CA-4) were synthesized and tested for their anti-proliferative activity. The highly diastereoselective acyl-Claisen rearrangement was used to provide 2,3-syn disubstituted morpholine amides which were used as precursors for the various analogues. This synthesis allows for the preparation of 1,2- and 2,3-diaryl-1H-pyrroles which are both geometrically similar to CA-4. These pyrrolic analogues were tested for their anti-proliferative activity against two human cell lines, K562 and MDA-MB-231 with 2,3-diaryl-1H-pyrrole 35 exhibiting the most potent activity with IC50 value of 0.07 μM against MDA-MB-231 cell line.
Cyclic nucleotide phosphodiesterase inhibitors, preparation and uses
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Page/Page column 22, (2010/11/08)
The invention concerns the use of PDE2 inhibitors for treating disorders of the central and peripheral nervous system, a method for therapeutic treatment by administering to an animal said inhibitors. More specifically, the invention concerns novel benzodiazepinone derivatives and their uses in therapeutics more particularly for treating pathologies involving activity of a cyclic nucleotide phosphodiesterase type 2. The invention also concerns methods for preparing same and novel synthesis intermediates.
