Replacement of pyrazol-3-yl amine hinge binder with thiazol-2-yl amine: Discovery of potent and selective JAK2 inhibitors |
| |
| Authors: | Stephanos Ioannidis Michelle L Lamb Lynsie Almeida Huiping Guan Bo Peng Geraldine Bebernitz Kirsten Bell Marat Alimzhanov Michael Zinda |
| |
| Institution: | 1. Department of Cancer Chemistry, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA;2. Department of Cancer Bioscience, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA |
| |
| Abstract: | Thiazol-2-yl amine was identified as an isosteric replacement for pyrazol-3-yl amine during our efforts to identify potent and selective JAK2 inhibitors. The rationale, synthesis and biological evaluation of several analogs is reported, along with the in vivo evaluation of the lead compounds. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
