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-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N8-neopentylpyrido[3,4- d]pyrimidine-2,8-diamine (BOS172722).
Woodward, H.L., Innocenti, P., Cheung, K.J., Hayes, A., Roberts, J., Henley, A.T., Faisal, A., Mak, G.W., Box, G., Westwood, I.M., Cronin, N., Carter, M., Valenti, M., De Haven Brandon, A., O'Fee, L., Saville, H., Schmitt, J., Burke, R., Broccatelli, F., van Montfort, R.L.M., Raynaud, F.I., Eccles, S.A., Linardopoulos, S., Blagg, J., Hoelder, S.
J. Med. Chem.
