On September 1, 2015, Gehling, Victor S.; Vaswani, Rishi G.; Nasveschuk, Christopher G.; Duplessis, Martin; Iyer, Priyadarshini; Balasubramanian, Srividya; Zhao, Feng; Good, Andrew C.; Campbell, Robert; Lee, Christina; Dakin, Les A.; Cook, Andrew S.; Gagnon, Alexandre; Harmange, Jean-Christophe; Audia, James E.; Cummings, Richard T.; Normant, Emmanuel; Trojer, Patrick; Albrecht, Brian K. published an article.Quality Control of Methyl 2-methyl-1H-indole-3-carboxylate The title of the article was Discovery, design, and synthesis of indole-based EZH2 inhibitors. And the article contained the following:
The discovery and optimization of a series of small mol. EZH2 inhibitors is described. Starting from dimethylpyridone HTS hit, a series of indole-based EZH2 inhibitors were identified. Biochem. potency and microsomal stability were optimized during these studies and afforded compound (I). Compound I demonstrates nanomolar levels of biochem. potency (IC50 = 0.002 μM), cellular potency (EC50 = 0.080 μM), and afforded tumor regression when dosed (200 mpk SC BID) in an EZH2 dependent tumor xenograft model. The experimental process involved the reaction of Methyl 2-methyl-1H-indole-3-carboxylate(cas: 65417-22-3).Quality Control of Methyl 2-methyl-1H-indole-3-carboxylate
The Article related to indole derivative preparation sar ezh2 inhibitor anticancer mao cell, ezh2, epigenetics, histone methyltransferase, prc2, pyridone, Pharmacology: Structure-Activity and other aspects.Quality Control of Methyl 2-methyl-1H-indole-3-carboxylate
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