Ontology highlight
ABSTRACT:
SUBMITTER: Vijayalakshmi N
PROVIDER: S-EPMC3197241 | biostudies-literature | 2010 Oct
REPOSITORIES: biostudies-literature
Bioconjugate chemistry 20101001 10
In this work, carboxyl-terminated PAMAM G-3.5 was covalently attached to SN38 via glycine and β-alanine spacers. The conjugates were stable at pH 7.4 and moderately hydrolyzed in cell culture media and rat plasma. Similarly to SN38 but to a lesser extent, both conjugates inhibited proliferation of human colorectal cancer HCT-116 cells, arrested the cell cycle in the G(2)/M phase, and led to nuclear fragmentation. However, activity of the conjugate with glycine spacer (IC(50) = 129 nM) was higher ...[more]