56436-24-9Relevant articles and documents
Cell-Based Drug Discovery: Identification and Optimization of Small Molecules that Reduce c-MYC Protein Levels in Cells
Berrodin, Thomas J.,Bhaskar, Aishwarya,Brackley, James,Butticello, Michael,Carpenter, Christopher,Di Marco, Christina,Heerding, Dirk A.,Kallal, Lorena A.,Lafrance, Louis,Li, William H.,Mack, James F.,Mangatt, Biju,Martyr, Cuthbert,McHugh, Charles,Minthorn, Elisabeth,Nartey, Eldridge N.,Rivero, Ralph,Rubin, Jacob,Suarez, Dominic,Tian, Xinrong,Medina, Jesús R.
, p. 16056 - 16087 (2021/11/10)
Elevated expression of the c-MYC oncogene is one of the most common abnormalities in human cancers. Unfortunately, efforts to identify pharmacological inhibitors that directly target MYC have not yet yielded a drug-like molecule due to the lack of any known small molecule binding pocket in the protein, which could be exploited to disrupt MYC function. We have recently described a strategy to target MYC indirectly, where a screening effort designed to identify compounds that can rapidly decrease endogenous c-MYC protein levels in a MYC-amplified cell line led to the discovery of a compound series that phenocopies c-MYC knockdown by siRNA. Herein, we describe our medicinal chemistry program that led to the discovery of potent, orally bioavailable c-MYC-reducing compounds. The development of a minimum pharmacophore model based on empirical structure activity relationship as well as the property-based approach used to modulate pharmacokinetics properties will be highlighted.
Copper catalyzed aerobic oxidative cyclization and ketonization: One pot synthesis of benzoimidazo[1,2-: A] imidazolones
Selvaraju, Manikandan,Ye, Tzuen-Yang,Li, Chia-Hsin,Ho, Pei-Heng,Sun, Chung-Ming
supporting information, p. 6621 - 6624 (2016/06/01)
A highly efficient synthesis of benzoimidazo[1,2-a]imidazolone through a novel oxidative 5-exo-dig cyclization-ketonization cascade of 2-aminobenzimidazole, aldehyde and terminal alkyne has been explored under aerobic conditions. The reaction proceeds thr
IMIDAZOLYL-IMIDAZOLES AS KINASE INHIBITORS
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Page/Page column 30, (2011/10/13)
Disclosed are compounds having the formula: wherein R1A, R1B, R2 and R3 are as defined herein, and methods of making and using the same.