944058-10-0Relevant academic research and scientific papers
Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor
Finlay, M. Raymond V.,Buttar, David,Critchlow, Susan E.,Dishington, Allan P.,Fillery, Shaun M.,Fisher, Eric,Glossop, Steve C.,Graham, Mark A.,Johnson, Trevor,Lamont, Gillian M.,Mutton, Simon,Perkins, Paula,Pike, Kurt G.,Slater., Anthony M.
scheme or table, p. 4163 - 4168 (2012/07/14)
High throughput screening to identify inhibitors of the mTOR kinase revealed sulfonyl-morpholino-pyrimidine 1 as an attractive start point. The compound displayed good physicochemical properties and selectivity over related kinases such as PI3Kα. Library preparation of related analogs allowed the establishment of additional SAR understanding and in particular the requirement for a key hydrogen bond donor motif at the 4-position of the phenyl ring in compounds such as indole 19. Isosteric replacement of the indole functionality led to the identification of urea compounds such as 32 that show good levels of mTOR inhibition in both enzyme and cellular assays.
COMPOUNDS 947
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Page/Page column 113, (2009/03/07)
A compound of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of proliferative disease such as cancer and partic
MORPHOLINO PYRIMIDINE DERIVATIVES AND THEIR USE IN THERAPY
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Page/Page column 152, (2008/06/13)
A compound of formula (I) or a salt, ester or prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by an mTOR kinase and/or one or more PI3K enzyme.
