Fragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors was written by Demont, Emmanuel H.;Chung, Chun-wa;Furze, Rebecca C.;Grandi, Paola;Michon, Anne-Marie;Wellaway, Chris;Barrett, Nathalie;Bridges, Angela M.;Craggs, Peter D.;Diallo, Hawa;Dixon, David P.;Douault, Clement;Emmons, Amanda J.;Jones, Emma J.;Karamshi, Bhumika V.;Locke, Kelly;Mitchell, Darren J.;Mouzon, Bernadette H.;Prinjha, Rab K.;Roberts, Andy D.;Sheppard, Robert J.;Watson, Robert J.;Bamborough, Paul. And the article was included in Journal of Medicinal Chemistry in 2015.COA of Formula: C10H13ClN2O2 This article mentions the following:
Overexpression of ATAD2 (ATPase family, AAA domain containing 2) has been linked to disease severity and progression in a wide range of cancers, and is implicated in the regulation of several drivers of cancer growth. Little is known of the dependence of these effects upon the ATAD2 bromodomain, which has been categorized as among the least tractable of its class. The absence of any potent, selective inhibitors limits clear understanding of the therapeutic potential of the bromodomain. Here, the authors describe the discovery of a hit from a fragment-based targeted array. Optimization of this produced the first known micromolar inhibitors of the ATAD2 bromodomain, e.g. I. In the experiment, the researchers used many compounds, for example, (2-Chloro-pyridin-3-yl)-carbamic acid tert-butyl ester (cas: 209798-48-1COA of Formula: C10H13ClN2O2).
(2-Chloro-pyridin-3-yl)-carbamic acid tert-butyl ester (cas: 209798-48-1) belongs to pyridine derivatives. Pyridine has a conjugated system of six π electrons that are delocalized over the ring. The molecule is planar and, thus, follows the Hückel criteria for aromatic systems. One of the examples of pyridines is the well-known alkaloid lithoprimidine, which is an A3 adenosine receptor antagonist and N,N-dimethylaminopyridine (DMAP) analog, commonly used in organic synthesis.COA of Formula: C10H13ClN2O2