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33. Ansideri F, Macedo JT, Eitel M, El-Gokha A, Zinad DS, Scarpellini C, Kudolo M,
Schollmeyer D, Boeckler FM, Blaum BS, Laufer SA, Koch P (2018) Structural optimization
of a Pyridinylimidazole scaffold: shifting the selectivity from p38α mitogen-activated protein
kinase to c-Jun N-terminal kinase 3. ACS Omega 3:7809–7831. https://doi.org/10.1021/
acsomega.8b00668
34. Muth F, El-Gokha A, Ansideri F, Eitel M, Döring E, Sievers-Engler A, Lange A, Boeckler FM,
Lämmerhofer M, Koch P, Laufer SA (2017) Tri- and tetrasubstituted pyridinylimidazoles as
covalent inhibitors of c-Jun N-terminal kinase 3. J Med Chem 60:594–607. https://doi.org/10.
1021/acs.jmedchem.6b01180
35. Koch P, Bäuerlein C, Jank H, Laufer S (2008) Activated Protein (MAP) kinase: synthesis
and biological testing of 2-Alkylsulfanyl-, 4(5)-aryl-, 5(4)-Heteroaryl-substituted Imidazoles.
J Med Chem 51:5630–5640. https://doi.org/10.1021/jm800373t
36. El-Gokha A, Laufer SA, Koch P (2015) An optimized and versatile synthesis to
pyridinylimidazole-type p38α mitogen activated protein kinase inhibitors. Org Biomol Chem
13:10699–10704. https://doi.org/10.1039/c5ob01505g
37. Zheng K, Iqbal S, Hernandez P, Park HJ, LoGrasso PV, Feng Y (2014) Design and synthesis
of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole
derivatives. J Med Chem 57:10013–10030. https://doi.org/10.1021/jm501256y
38. Singh J, Petter RC, Baillie TA, Whitty A (2011) The resurgence of covalent drugs. Nat Rev
Drug Discov 10:307–317. https://doi.org/10.1038/nrd3410
39. Liu QS, Sabnis Y, Zhao Z, Zhang TH, Buhrlage SJ, Jones LH, Gray NS (2013) Developing
irreversible inhibitors of the protein kinase cysteinome. Chem Biol 20:146–159. https://doi.org/
10.1016/j.chembiol.2012.12.006
40. Chaikuad A, Koch P, Laufer SA, Knapp S (2018) The cysteinome of protein kinases as a
target in drug development. Angew Chem Int Ed 57:4372–4385. https://doi.org/10.1002/anie.
201707875
41. Nagar B, Bornmann WG, Pellicena P, Schindler T, Veach DR, Miller WT, Clarkson B,
Kuriyan J (2002) Crystal structures of the kinase domain of c-Abl in complex with the
small molecule inhibitors PD173955 and imatinib (STI-571). Cancer Res 62:4236–4243
224
P. Koch
relation to p38α MAPK. Molecules 22:522. https://doi.org/10.3390/molecules22040522
33. Ansideri F, Macedo JT, Eitel M, El-Gokha A, Zinad DS, Scarpellini C, Kudolo M,
Schollmeyer D, Boeckler FM, Blaum BS, Laufer SA, Koch P (2018) Structural optimization
of a Pyridinylimidazole scaffold: shifting the selectivity from p38α mitogen-activated protein
kinase to c-Jun N-terminal kinase 3. ACS Omega 3:7809–7831. https://doi.org/10.1021/
acsomega.8b00668
34. Muth F, El-Gokha A, Ansideri F, Eitel M, Döring E, Sievers-Engler A, Lange A, Boeckler FM,
Lämmerhofer M, Koch P, Laufer SA (2017) Tri- and tetrasubstituted pyridinylimidazoles as
covalent inhibitors of c-Jun N-terminal kinase 3. J Med Chem 60:594–607. https://doi.org/10.
1021/acs.jmedchem.6b01180
35. Koch P, Bäuerlein C, Jank H, Laufer S (2008) Activated Protein (MAP) kinase: synthesis
and biological testing of 2-Alkylsulfanyl-, 4(5)-aryl-, 5(4)-Heteroaryl-substituted Imidazoles.
J Med Chem 51:5630–5640. https://doi.org/10.1021/jm800373t
36. El-Gokha A, Laufer SA, Koch P (2015) An optimized and versatile synthesis to
pyridinylimidazole-type p38α mitogen activated protein kinase inhibitors. Org Biomol Chem
13:10699–10704. https://doi.org/10.1039/c5ob01505g
37. Zheng K, Iqbal S, Hernandez P, Park HJ, LoGrasso PV, Feng Y (2014) Design and synthesis
of highly potent and isoform selective JNK3 inhibitors: SAR studies on aminopyrazole
derivatives. J Med Chem 57:10013–10030. https://doi.org/10.1021/jm501256y
38. Singh J, Petter RC, Baillie TA, Whitty A (2011) The resurgence of covalent drugs. Nat Rev
Drug Discov 10:307–317. https://doi.org/10.1038/nrd3410
39. Liu QS, Sabnis Y, Zhao Z, Zhang TH, Buhrlage SJ, Jones LH, Gray NS (2013) Developing
irreversible inhibitors of the protein kinase cysteinome. Chem Biol 20:146–159. https://doi.org/
10.1016/j.chembiol.2012.12.006
40. Chaikuad A, Koch P, Laufer SA, Knapp S (2018) The cysteinome of protein kinases as a
target in drug development. Angew Chem Int Ed 57:4372–4385. https://doi.org/10.1002/anie.
201707875
41. Nagar B, Bornmann WG, Pellicena P, Schindler T, Veach DR, Miller WT, Clarkson B,
Kuriyan J (2002) Crystal structures of the kinase domain of c-Abl in complex with the
small molecule inhibitors PD173955 and imatinib (STI-571). Cancer Res 62:4236–4243
224
P. Koch