LCRF-0004的受限类似物作为有效的RON酪氨酸激酶抑制剂的设计与合成。
Design and synthesis of constrained analogs of LCRF-0004 as potent RON tyrosine kinase inhibitors.
作者信息
Raeppel Stéphane L, Therrien Eric, Raeppel Franck
机构信息
Laboratoires ChemRF Inc. / ChemRF Laboratories Inc., 3194 rue Claude-Jodoin, Montréal, QC H1Y 3M2, Canada.
Laboratoires ChemRF Inc. / ChemRF Laboratories Inc., 3194 rue Claude-Jodoin, Montréal, QC H1Y 3M2, Canada.
出版信息
Bioorg Med Chem Lett. 2015 Sep 1;25(17):3706-10. doi: 10.1016/j.bmcl.2015.06.034. Epub 2015 Jun 15.
New fused bicyclic lactam head groups as rigidified analogs of thieno[3,2-b]pyridine-based kinase inhibitor LCRF-0004 were designed and synthesized. Depending on the functionalities and the size of these bicyclic head groups, potent inhibitors of RON tyrosine kinase with various level of selectivity against c-Met tyrosine kinase were obtained.
设计并合成了新型稠合双环内酰胺头部基团，作为基于噻吩并[3,2-b]吡啶的激酶抑制剂LCRF-0004的刚性类似物。根据这些双环头部基团的功能和大小，获得了对RON酪氨酸激酶具有强效抑制作用且对c-Met酪氨酸激酶具有不同选择性水平的抑制剂。
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