Ontology highlight
ABSTRACT:
SUBMITTER: Kraus GA
PROVIDER: S-EPMC3891048 | biostudies-literature | 2010 Sep
REPOSITORIES: biostudies-literature
Kraus George A GA Gupta Vinayak V Mokhtarian Marjan M Mehanovic Samir S Nilsen-Hamilton Marit M
Bioorganic & medicinal chemistry 20100714 17
The effects of substituents on the aryl ring were studied by the preparation and testing of several PD173955 analogs. Inserting a single carbon atom into the C-N bond in the aniline subunit (PDC) reduced the kinase inhibition by a factor of 200. Despite its decreased affinity for Abl compared with PD173955, PDC exhibits a Ki very similar to that reported for Imatinib. Increased water solubility is also gained by replacing the thiomethyl group with an amino or glycyl moiety. For both PD173955 and ...[more]