Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases.

Casuscelli, Francesco; Ardini, Elena; Avanzi, Nilla; Casale, Elena; Cervi, Giovanni; D'Anello, Matteo; Donati, Daniele; Faiardi, Daniela; Ferguson, Ronald D; Fogliatto, Gianpaolo; Galvani, Arturo; Marsiglio, Aurelio; Mirizzi, Danilo G; Montemartini, Marisa; Orrenius, Christian; Papeo, Gianluca; Piutti, Claudia; Salom, Barbara; Felder, Eduard R

Casuscelli, Francesco; Ardini, Elena; Avanzi, Nilla; Casale, Elena; Cervi, Giovanni; D'Anello, Matteo; Donati, Daniele; Faiardi, Daniela; Ferguson, Ronald D; Fogliatto, Gianpaolo; Galvani, Arturo; Marsiglio, Aurelio; Mirizzi, Danilo G; Montemartini, Marisa; Orrenius, Christian; Papeo, Gianluca; Piutti, Claudia; Salom, Barbara; Felder, Eduard R.

Affiliation

Casuscelli F; Oncology, Nerviano Medical Sciences, viale Pasteur 10, 20014 Nerviano (MI), Italy. Electronic address: francesco.casuscelli@nervianoms.com.

Bioorg Med Chem ; 21(23): 7364-80, 2013 Dec 01.

Article in En | MEDLINE | ID: mdl-24139169

Subject(s)

Protein Kinase Inhibitors/chemistry; Protein Kinase Inhibitors/pharmacology; Proto-Oncogene Proteins c-pim-1/antagonists & inhibitors; Pyrazines/chemistry; Pyrazines/pharmacology; Drug Discovery; Humans; Molecular Docking Simulation; Protein Kinase Inhibitors/chemical synthesis; Protein Structure, Tertiary; Proto-Oncogene Proteins c-pim-1/chemistry; Proto-Oncogene Proteins c-pim-1/metabolism; Pyrazines/chemical synthesis

Key words

Anti-cancer agents; Kinase selectivity; Natural product scaffold; PIM kinases; Pyrrolopyrazinone

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Full text: 1 Database: MEDLINE Main subject: Pyrazines / Protein Kinase Inhibitors / Proto-Oncogene Proteins c-pim-1 Limits: Humans Language: En Year: 2013 Type: Article

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Full text: 1 Database: MEDLINE Main subject: Pyrazines / Protein Kinase Inhibitors / Proto-Oncogene Proteins c-pim-1 Limits: Humans Language: En Year: 2013 Type: Article