Tosso, Perrer N. et al. published their research in Journal of Medicinal Chemistry in 2014 | CAS: 15540-90-6

4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Application of 15540-90-6

Synthesis and Structure-Activity Relationship Studies of Small Molecule Disruptors of EWS-FLI1 Interactions in Ewing’s Sarcoma was written by Tosso, Perrer N.;Kong, Yali;Scher, Lauren;Cummins, Ryan;Schneider, Jeffrey;Rahim, Said;Holman, K. Travis;Toretsky, Jeffrey;Wang, Kan;Uren, Aykut;Brown, Milton L.. And the article was included in Journal of Medicinal Chemistry in 2014.Application of 15540-90-6 The following contents are mentioned in the article:

EWS-FLI1 is an oncogenic fusion protein implicated in the development of Ewing’s sarcoma family tumors (ESFT). Using the previously reported lead compound I, the authors designed and synthesized a focused library of analogs. The functional inhibition of the analogs was measured by an EWS-FLI1/NR0B1 reporter luciferase assay and a paired cell screening approach measuring effects on growth inhibition for human cells containing EWS-FLI1 (TC32 and TC71) and control PANC1 cell lines devoid of the oncoprotein. The data revealed that substitution of electron donating groups at the para-position on the Ph ring was the most favorable for inhibition of EWS-FLI1 by analogs of I. Compound II was the most active inhibitor with GI50 = 0.26±0.1 μM. Further, a correlation of growth inhibition (EWS-FLI1 expressing TC32 cells) and the luciferase reporter activity was established (R2 = 0.84). Finally, the authors designed and synthesized a biotinylated analog and determined the binding affinity for recombinant EWS-FLI1 (Kd = 4.8±2.6 μM). This study involved multiple reactions and reactants, such as 4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6Application of 15540-90-6).

4,7-Dimethylindoline-2,3-dione (cas: 15540-90-6) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Application of 15540-90-6

Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles