|
|||||
|
|
Structure and activity relationships of tartrate-based TACE inhibitors |
|
| Authors: | Dansu Li Janeta Popovici-Muller David B. Belanger John Caldwell Chaoyang Dai Maria David Vinay M. Girijavallabhan Brian J. Lavey Joe F. Lee Zhidan Liu Rob Mazzola Razia Rizvi Kristin E. Rosner Bandarpalle Shankar Jim Spitler Pauline C. Ting Henry Vaccaro Wensheng Yu Guowei Zhou Zhaoning Zhu Corey O. Strickland |
| Affiliation: | 1. Department of Medicinal Chemistry, Merck Research Laboratories, Cambridge, 320 Bent Street, Cambridge, MA 02141, United States;2. Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States;3. Department of Inflammation, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States |
| Abstract: | The syntheses and structure–activity relationships of the tartrate-based TACE inhibitors are discussed. The optimization of both the prime and non-prime sites led to compounds with picomolar activity. Several analogs demonstrated good rat pharmacokinetics. |
| Keywords: | |
| 本文献已被 ScienceDirect 等数据库收录！ | |