Scott David A, Aquila Brian M, Bebernitz Geraldine A, Cook Donald J, Dakin Les A, Deegan Tracy L, Hattersley Maureen M, Ioannidis Stephanos, Lyne Paul D, Omer Charles A, Ye Minwei, Zheng Xiaolan
Cancer Research, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA.
Bioorg Med Chem Lett. 2008 Sep 1;18(17):4794-7. doi: 10.1016/j.bmcl.2008.07.093. Epub 2008 Jul 27.
The bisamide class of kinase inhibitors was identified as being active against CSF-1R. The synthesis and SAR of pyridyl and thiazolyl bisamides are reported, along with the pharmacokinetic properties and in vivo activity of selected examples.
双酰胺类激酶抑制剂被确定对集落刺激因子1受体(CSF-1R)具有活性。本文报道了吡啶基和噻唑基双酰胺的合成、构效关系,以及所选实例的药代动力学性质和体内活性。