918492-64-5Relevant articles and documents
Fragment-Based Drug Discovery of Potent Protein Kinase C Iota Inhibitors
Kwiatkowski, Jacek,Liu, Boping,Tee, Doris Hui Ying,Chen, Guoying,Ahmad, Nur Huda Binte,Wong, Yun Xuan,Poh, Zhi Ying,Ang, Shi Hua,Tan, Eldwin Sum Wai,Ong, Esther Hq,Nurul, Dinie,Poulsen, Anders,Pendharkar, Vishal,Sangthongpitag, Kanda,Lee, May Ann,Sepramaniam, Sugunavathi,Ho, Soo Yei,Cherian, Joseph,Hill, Jeffrey,Keller, Thomas H.,Hung, Alvin W.
, p. 4386 - 4396 (2018)
Protein kinase C iota (PKC-i) is an atypical kinase implicated in the promotion of different cancer types. A biochemical screen of a fragment library has identified several hits from which an azaindole-based scaffold was chosen for optimization. Driven by a structure-activity relationship and supported by molecular modeling, a weakly bound fragment was systematically grown into a potent and selective inhibitor against PKC-i.
ISOQUINOLINE DERIVATIVES AS INHIBITORS OF RHO-KINASE
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Page/Page column 32-33, (2008/06/13)
The invention relates to 6-piperidinyl-substituted isoquinoline derivatives of the formula (I); useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.