Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N(2)-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N(8)-neopentylpyrido[3,4- d]pyrimidine-2,8-diamine (BOS172722)
引入甲基可抑制吡啶并[3,4-d]嘧啶单极纺锤体1 (MPS1) 抑制剂的代谢，并促成了 1 期临床候选药物 N(2)-(2-乙氧基-4-(4-甲基-4H-1,2,4-三唑-3-基)苯基)-6-甲基-N(8)-新戊基吡啶并[3,4-d]嘧啶-2,8-二胺 (BOS172722) 的发现。
期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/acs.jmedchem.8b00690
Woodward, Hannah L; Innocenti, Paolo; Cheung, Kwai-Ming J; Hayes, Angela; Roberts, Jennie; Henley, Alan T; Faisal, Amir; Mak, Grace Wing-Yan; Box, Gary; Westwood, Isaac M; Cronin, Nora; Carter, Michael; Valenti, Melanie; De Haven Brandon, Alexis; O'Fee, Lisa; Saville, Harry; Schmitt, Jessica; Burke, Rosemary; Broccatelli, Fabio; van Montfort, Rob L M; Raynaud, Florence I; Eccles, Suzanne A; Linardopoulos, Spiros; Blagg, Julian; Hoelder, Swen
