143218-46-6Relevant articles and documents
Indole RSK inhibitors. Part 2: Optimization of cell potency and kinase selectivity
Kirrane, Thomas M.,Boyer, Stephen J.,Burke, Jennifer,Guo, Xin,Snow, Roger J.,Soleymanzadeh, Lida,Swinamer, Alan,Zhang, Yunlong,Madwed, Jeffery B.,Kashem, Mohammed,Kugler, Stanley,O'Neill, Margaret M.
scheme or table, p. 738 - 742 (2012/03/11)
A series of inhibitors for the 90 kDa ribosomal S6 kinase (RSK) based on an 1-oxo-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide scaffold were optimized for cellular potency and kinase selectivity. This led to the identification of compound 24, BIX 02565, an attractive candidate for use in vitro and in vivo to explore the role of RSK as a target for the treatment heart failure.
Azolyl methyl phenyl derivatives having aromatase inhibitory activity
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, (2008/06/13)
Compounds exerting excellent aromatase inhibitory activity in vivo and in vitro with higher specificity and greater safety are provided together with the salts thereof. Using the same, there are also provided, prophylactic agents and/or therapeutical agents of estrogen-dependent diseases, contraceptive agents for females, and aromatase inhibitory agents for use in the form of reagents for human or animals. The compounds are of the formula (I), wherein R2 is represented by the formula (II) or (III). (I) (II) or