Medina, Jesus R.; Tian, Xinrong; Li, William H.; Suarez, Dominic; Mack, James F.; LaFrance, Louis; Martyr, Cuthbert; Brackley, James; Di Marco, Christina; Rivero, Ralph; Heerding, Dirk A.; McHugh, Charles; Minthorn, Elisabeth; Bhaskar, Aishwarya; Rubin, Jacob; Butticello, Michael; Carpenter, Christopher; Nartey, Eldridge N.; Berrodin, Thomas J.; Kallal, Lorena A.; Mangatt, Biju published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Cell-Based Drug Discovery: Identification and Optimization of Small Molecules that Reduce c-MYC Protein Levels in Cells》.Recommanded Product: Methyl 4-fluoro-3-nitrobenzoate The article contains the following contents:
Elevated expression of the c-MYC oncogene is one of the most common abnormalities in human cancers. Unfortunately, efforts to identify pharmacol. inhibitors that directly target MYC have not yet yielded a drug-like mol. due to the lack of any known small mol. 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 chem. program that led to the discovery of potent, orally bioavailable c-MYC-reducing compounds The development of a min. pharmacophore model based on empirical structure activity relationship as well as the property-based approach used to modulate pharmacokinetics properties will be highlighted. The experimental part of the paper was very detailed, including the reaction process of Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9Recommanded Product: Methyl 4-fluoro-3-nitrobenzoate)
Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9) belongs to methyl benzoate. Methyl benzoate reacts at both the ring and the ester, depending on the substrate. Electrophiles attack the ring, illustrated by acid-catalysed nitration with nitric acid to give methyl 3-nitrobenzoate.Recommanded Product: Methyl 4-fluoro-3-nitrobenzoateMethyl 4-fluoro-3-nitrobenzoate is used to prepare dimethyl 3-nitro-3′,4-oxydibenzoate by reacting with 3-hydroxy-benzoic acid methyl ester.
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Ester – an overview | ScienceDirect Topics