1610045-39-0Relevant academic research and scientific papers
Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models
Winter-Holt, Jon J.,Bardelle, Catherine,Chiarparin, Elisabetta,Dale, Ian L.,Davey, Paul R. J.,Davies, Nichola L.,Denz, Christopher,Fillery, Shaun M.,Guérot, 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
, p. 3306 - 3331 (2022/02/23)
ATAD2 is an epigenetic bromodomain-containing target which is overexpressed in many cancers and has been suggested as a potential oncology target. While several small molecule 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), a highly potent and selective ATAD2 inhibitor which shows cellular target engagement and antiproliferative activity in a range of breast cancer models.
COMBINATION TREATMENT OF ACUTE MYELOID LEUKEMIA
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Page/Page column 20; 37, (2019/08/12)
The present invention relates to the use of volasertib, or a pharmaceutically acceptable salt thereof or a hydrate thereof, in combination with a BET inhibitor, or a pharmaceutically acceptable salt thereof or a hydrate thereof for treating patients suffering from acute myeloid leukemia (AML).
Triazolopyrazine
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Paragraph 0303; 0304; 0305, (2015/05/26)
The present invention encompasses compounds of general formula (I) wherein the groups R1 to R3, X3 to X6 have the meanings given in the claims and in the specification. The compounds of the invention are suitabl
TRIAZOLOPYRAZINE DERIVATIVES AS BRD4 INHIBITORS
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Page/Page column 42, (2015/05/26)
The present invention encompasses compounds of general formula (I), wherein the groups R1 to R3, X3 to X6 have the meanings given in the claims and in the specification. The compounds of the invention are suitab
TRIAZOLOPYRAZINE
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Paragraph 0249 - 0252, (2014/05/25)
Disclosed are compounds of the formula (I) wherein the groups R1 to R3 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
