Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models was written by Winter-Holt, Jon J.;Bardelle, Catherine;Chiarparin, Elisabetta;Dale, Ian L.;Davey, Paul R. J.;Davies, Nichola L.;Denz, Christopher;Fillery, Shaun M.;Guerot, Carine M.;Han, Fujin;Hughes, Samantha J.;Kulkarni, Meghana;Liu, Zhaoqun;Milbradt, Alexander;Moss, Thomas A.;Niu, Huijun;Patel, Joe;Rabow, Alfred A.;Schimpl, Marianne;Shi, Junjie;Sun, Dongqing;Yang, Dejian;Guichard, Sylvie. And the article was included in Journal of Medicinal Chemistry in 2022.Synthetic Route of C7H5ClN2O4 This article mentions the following:
ATAD2 is an epigenetic bromodomain-containing target which is overexpressed in many cancers and has been suggested as a potential oncol. target. While several small mol. inhibitors have been described in the literature, their cellular activity has proved to be underwhelming. In this work, we describe the identification of a novel series of ATAD2 inhibitors by high throughput screening, confirmation of the bromodomain region as the site of action, and the optimization campaign undertaken to improve the potency, selectivity, and permeability of the initial hit. The result is compound 5 (AZ13824374)(I), a highly potent and selective ATAD2 inhibitor which shows cellular target engagement and antiproliferative activity in a range of breast cancer models. In the experiment, the researchers used many compounds, for example, Methyl 6-chloro-5-nitronicotinate (cas: 59237-53-5Synthetic Route of C7H5ClN2O4).
Methyl 6-chloro-5-nitronicotinate (cas: 59237-53-5) belongs to organic chlorides. Organic chlorides can cause corrosion in pipelines, valves and condensers, and cause catalyst poisoning. The hydrocarbon processing industry (HPI) and others are affected by damage caused by these substances. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.Synthetic Route of C7H5ClN2O4
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics