Ontology highlight
ABSTRACT:
SUBMITTER: Sala M
PROVIDER: S-EPMC7127540 | biostudies-literature | 2016 Jun
REPOSITORIES: biostudies-literature
Šála Michal M Kögler Martin M Plačková Pavla P Mejdrová Ivana I Hřebabecký Hubert H Procházková Eliška E Strunin Dmytro D Lee Gary G Birkus Gabriel G Weber Jan J Mertlíková-Kaiserová Helena H Nencka Radim R
Bioorganic & medicinal chemistry letters 20160405 11
We report on an extensive structure-activity relationship study of novel PI4K IIIβ inhibitors. The purine derivative of the potent screening hit T-00127-HEV1 has served as a suitable starting point for a thorough investigation of positions 8 and 2. While position 8 of the purine scaffold can only bear a small substituent to maintain the inhibitory activity, position 2 is opened for extensive modification and can accommodate even substituted phenyl rings without the loss of PI4K IIIβ inhibitory a ...[more]