Authors Voller, J; Zahajska, L; Plihalova, L; Jerabkova, J; Burget, D; Pataki, AC; Krystof, V; Zatloukal, M; Brabek, J; Rosel, D; Mik, V; Tkac, M; Pospisil, T; Gucky, T; Dolezal, K; Strnad, M in ACADEMIC PRESS INC ELSEVIER SCIENCE published article about RHO KINASE INHIBITORS; CELL-MIGRATION; HEPATOCELLULAR-CARCINOMA; AMEBOID INVASIVENESS; THERAPEUTIC TARGET; MYOSIN-II; GTPASES; METASTASIS; ACTIVATION; INVASION in [Voller, Jiri; Plihalova, Lucie; Jerabkova, Jana; Burget, David; Krystof, Vladimir; Tkac, Martin; Dolezal, Karel; Strnad, Miroslav] Czech Acad Sci, Inst Expt Bot, Lab Growth Regulators, Slechtitelu 27, CZ-78371 Olomouc, Czech Republic; [Voller, Jiri; Plihalova, Lucie; Jerabkova, Jana; Burget, David; Krystof, Vladimir; Tkac, Martin; Dolezal, Karel; Strnad, Miroslav] Palacky Univ, Slechtitelu 27, CZ-78371 Olomouc, Czech Republic; [Voller, Jiri] Palacky Univ, Fac Med & Dent, Inst Mol & Translat Med, Dept Clin & Mol Pathol, Hnevotinska 3, Olomouc 77515, Czech Republic; [Zahajska, Lenka] Czech Acad Sci, Inst Expt Bot, Isotope Lab, Videnska 1083, Prague 14200 4, Czech Republic; [Plihalova, Lucie; Zatloukal, Marek; Mik, Vaclav; Pospisil, Tomas; Gucky, Tomas; Dolezal, Karel] Palacky Univ, Ctr Reg Hana Biotechnol & Agr Res, Dept Chem Biol & Genet, Slechtitelu 27, CZ-78371 Olomouc, Czech Republic; [Pataki, Andreea Csilla; Brabek, Jan; Rosel, Daniel] Charles Univ Prague, Fac Sci, Dept Cell Biol, Vinicna 7, Prague 12843 2, Czech Republic in 2019, Cited 50. Safety of 1,4-Dioxa-8-azaspiro[4.5]decane. The Name is 1,4-Dioxa-8-azaspiro[4.5]decane. Through research, I have a further understanding and discovery of 177-11-7
Rho-associated serine/threonine kinases (ROCKs) are principal regulators of the actin cytoskeleton that regulate the contractility, shape, motility, and invasion of cells. We explored the relationships between structure and anti-ROCK2 activity in a group of purine derivatives substituted at the C6 atom by piperidin-1-yl or azepan-1-yl groups. Structure-activity relationship (SAR) analyses suggested that anti-ROCK activity is retained, and may be further increased, by substitution of the parent compounds at the C2 atom or by expansion of the C6 side chain. These inhibitors of ROCK can reach effective concentrations within cells, as demonstrated by a decrease in phosphorylation of the ROCK target MLC, and by inhibition of the ROCK-dependent invasion of melanoma cells in the collagen matrix. Our study may be useful for further optimization of C6-substituted purine inhibitors of ROCKs and of other sensitive kinases identified by the screening of a broad panel of protein kinases.
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Reference：
Piperidine – Wikipedia,
Piperidine | C5H7510N – PubChem