33089-15-5Relevant articles and documents
SPAK/OSR INHIBITORS AND METHODS OF USING SAME
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Page/Page column 59-60, (2021/06/11)
The present disclosure provides SPAK/OSR inhibitors. In certain embodiments, the compounds of the disclosure can be used to treat, ameliorate, and/or prevent certain cancers in a subject.
Discovery of N6-phenyl-1H-pyrazolo[3,4-d]pyrimidine-3,6-diamine derivatives as novel CK1 inhibitors using common-feature pharmacophore model based virtual screening and hit-to-lead optimization
Yang, Ling-Ling,Li, Guo-Bo,Yan, Heng-Xiu,Sun, Qi-Zheng,Ma, Shuang,Ji, Pan,Wang, Ze-Rong,Feng, Shan,Zou, Jun,Yang, Sheng-Yong
, p. 30 - 38 (2013/01/15)
Aberrant activation of casein kinase 1 (CK1) has been demonstrated to be implicated in the pathogenesis of cancer and various central nervous system disorders. Discovery of CK1 inhibitors has thus attracted much attention in recent years. In this account, we describe the discovery of N6-phenyl-1H- pyrazolo[3,4-d]pyrimidine-3,6-diamine derivatives as novel CK1 inhibitors. An optimal common-feature pharmacophore hypothesis, termed Hypo2, was firstly generated, followed by virtual screening using Hypo2 against several chemical databases. One of the best hit compounds, N6-(4-chlorophenyl)-1H-pyrazolo[3,4-d] pyrimidine-3,6-diamine, was chosen for the subsequent hit-to-lead optimization under the guide of Hypo2, which led to the discovery of a new lead compound (1-(3-(3-amino-1H-pyrazolo[3,4-d]pyrimidin-6-ylamino)phenyl)-3-(3-chloro-4- fluorophenyl)urea) that potently inhibits CK1 with an IC50 value of 78 nM.
Pyrimidinyl pyridone inhibitors of kinases
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Page/Page column 43-44, (2009/10/31)
This application discloses novel pyrimidinyl pyridone derivatives according to formula I, wherein A, R1, R2, R3, and m are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modula
Thrombin inhibitors
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, (2008/06/13)
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: wherein R1 is, for example, hydrogen, Cl, or cyano, and R2 is, for example, hydrogen,
N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists
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, (2019/08/08)
Compounds represented by Formula (I): 1or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
