19157-84-7Relevant academic research and scientific papers
Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8
Bergeron, Philippe,Koehler, Michael F. T.,Blackwood, Elizabeth M.,Bowman, Krista,Clark, Kevin,Firestein, Ron,Kiefer, James R.,Maskos, Klaus,McCleland, Mark L.,Orren, Linda,Ramaswamy, Sreemathy,Salphati, Laurent,Schmidt, Steve,Schneider, Elisabeth V.,Wu, Jiansheng,Beresini, Maureen
supporting information, p. 595 - 600 (2016/07/06)
Using Sorafenib as a starting point, a series of potent and selective inhibitors of CDK8 was developed. When cocrystallized with CDK8 and cyclin C, these compounds exhibit a Type-II (DMG-out) binding mode.
2,4-Pyrimidinediamine Compounds and Their Uses
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Paragraph 1034; 1035, (2015/11/10)
The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
Potent and subtype-selective CCK-B/gastrin receptor antagonists: 2,4-dioxo-1,5-benzodiazepines with a plane of symmetry
Hagishita, Sanji,Seno, Kaoru,Kamata, Susumu,Haga, Nobuhiro,Ishihara, Yasunobu,Ishikawa, Michio,Shimamura, Mayumi
, p. 1433 - 1446 (2007/10/03)
A series of CCK-B/gastrin receptor antagonists, 2,4-dioxo-1,5-benzodiazepine derivatives with a plane of symmetry, were designed, synthesized, and evaluated for antagonistic activity. Structure-activity relationship studies revealed that carbonylmethyl groups at both N-1 and N-5 positions and hydrophilic groups, such as the carboxyl group on the benzene ring attached to the ureido group at the C-3 position, brought about potent affinity and subtype selectivity for CCK-B/gastrin receptors. Several compounds showed excellent in vivo inhibition of gastric acid secretion induced by pentagastrin in anesthetized rats.
Method of inhibiting sickling of sickle erythrocytes
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, (2008/06/13)
Method for inhibiting the sickling of sickle erythrocytes in blood by contacting the sickle erythrocytes with a compound of the formula: STR1 or a pharmaceutically-acceptable salt thereof wherein X represents sulfur, oxygen or imino; and Rm and Rp each independently represent hydrogen, cyano, nitro, alkylthio, alkylsulfinyl, alkylsulfonyl, alkyl or trifluoromethyl.
