Ontology highlight
ABSTRACT:
SUBMITTER: Nakano H
PROVIDER: S-EPMC5430388 | biostudies-literature | 2017 May
REPOSITORIES: biostudies-literature
Nakano Hirofumi H Hasegawa Tsukasa T Kojima Hirotatsu H Okabe Takayoshi T Nagano Tetsuo T
ACS medicinal chemistry letters 20170403 5
In the development of kinase inhibitors, one of the major concerns is selectivity. An effective strategy to achieve high selectivity is to utilize structural differences among kinases to inform inhibitor design. Here, we set out to improve the PIM (proviral integration site for Moloney murine leukemia virus) kinase-inhibitory selectivity of our previously reported 7-azaindole derivative <b>2</b>, which has promising ADMET properties, by targeting a unique bulge in the ATP-binding pocket. 6-Subst ...[more]