Liang, Rui published the artcileA Chemical Strategy toward Novel Brain-Penetrant EZH2 Inhibitors, HPLC of Formula: 3032-32-4, the main research area is EZH2 inhibitor anticancer blood brain barrier metabolic stability.
Aberrant gene-silencing through dysregulation of polycomb protein activity has emerged as an important oncogenic mechanism in cancer, implicating polycomb proteins as important therapeutic targets. Recently, an inhibitor targeting EZH2, the methyltransferase component of PRC2, received U.S. Food and Drug Administration approval following promising clin. responses in cancer patients. However, the current array of EZH2 inhibitors have poor brain penetrance, limiting their use in patients with central nervous system malignancies, a number of which have been shown to be sensitive to EZH2 inhibition. To address this need, we have identified a chem. strategy, based on computational modeling of pyridone-containing EZH2 inhibitor scaffolds, to minimize P-glycoprotein activity, and here we report the first brain-penetrant EZH2 inhibitor, TDI-6118 (compound 5). Addnl., in the course of our attempts to optimize this compound, we discovered TDI-11904 (compound 21), a novel, highly potent, and peripherally active EZH2 inhibitor based on a 7 member ring structure.
ACS Medicinal Chemistry Letters published new progress about Antiproliferative agents. 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, HPLC of Formula: 3032-32-4.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics