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 N2-(2-Ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N8-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine (BOS172722)

Woodward, HL; Innocenti, P; Cheung, KMJ; Hayes, A; Roberts, J; Henley, AT; Faisal, A; ... Hoelder, S; + view all Woodward, HL; Innocenti, P; Cheung, KMJ; Hayes, A; Roberts, J; Henley, AT; Faisal, A; Mak, GWY; Box, G; Westwood, IM; Cronin, N; Carter, M; Valenti, M; De Haven Brandon, A; O'Fee, L; Saville, H; Schmitt, J; Burke, R; Broccatelli, F; Van Montfort, RLM; Raynaud, FI; Eccles, SA; Linardopoulos, S; Blagg, J; Hoelder, S; - view fewer (2018) 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 N2-(2-Ethoxy-4-(4-methyl-4H-1,2,4-triazol-3-yl)phenyl)-6-methyl-N8-neopentylpyrido[3,4-d]pyrimidine-2,8-diamine (BOS172722). Journal of Medicinal Chemistry , 61 (18) pp. 8226-8240. 10.1021/acs.jmedchem.8b00690 . Green open access

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