856290-28-3Relevant articles and documents
ARYL HYDROCARBON RECEPTOR (AHR) ACTIVATOR COMPOUNDS AS CANCER THERAPEUTICS
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Page/Page column 84, (2020/06/05)
The present disclosure relates to compositions and methods for the diagnosis and treatment or prevention of cancers, particularly cancers that exhibit elevated expression of FOXA1 and/or FOXA1 gene targets, such as certain breast, liver and/or prostate cancers, including luminal and/or ER-positive forms of breast cancer. Three previously identified adenosine receptor antagonists, CGS-15943, MRS-1220 and SCH-58261, as well as furan ring moiety-possessing derivatives of CGS-15943 are specifically provided for killing cancer cells in a manner that appears to involve activation of the aryl hydrocarbon receptor (AHR) by such compounds. The instant disclosure therefore provides for selecting and/or administering CGS-15943, MRS-1220, SCH-58261 and/or a furan-possessing derivative of CGS-15943, MRS-1220 and/or SCH-58261 as a therapeutic agent to target a cancer cell and/or subject having or at risk of developing a cancer. Methods and compositions for therapies that include such compounds are also provided
2,6-Diaryl-4-phenacylaminopyrimidines as potent and selective adenosine A2A antagonists with reduced hERG liability
Moorjani, Manisha,Zhang, Xiaohu,Chen, Yongsheng,Lin, Emily,Rueter, Jaimie K.,Gross, Raymond S.,Lanier, Marion C.,Tellew, John E.,Williams, John P.,Lechner, Sandra M.,Malany, Siobhan,Santos, Mark,Ekhlassi, Paddi,Castro-Palomino, Julio C.,Crespo, Maria I.,Prat, Maria,Gual, Silvia,Diaz, Jose-Luis,Saunders, John,Slee, Deborah H.
, p. 1269 - 1273 (2008/09/18)
In this report, the design and synthesis of a series of pyrimidine based adenosine A2A antagonists are described. The strategy and outcome of expanding SAR exploration to attenuate hERG and improve selectivity over A1 are discussed.
