Ontology highlight
ABSTRACT:
SUBMITTER: Wang SB
PROVIDER: S-EPMC4554882 | biostudies-literature | 2015 Sep
REPOSITORIES: biostudies-literature
Bioorganic & medicinal chemistry 20150717 17
Thirteen new N-aryl 1,2,3,4-tetrahydroquinoline compounds (4a-f, 6a-c, and 8a-d) were synthesized and evaluated for antitumor activity and drug-like properties. Compound 4a exhibited high inhibitory potency with low nanomolar GI50 values of 16-20 nM in cellular assays, including excellent activity against the P-glycoprotein overexpressing cell line KBvin. Compound 4a inhibited colchicine binding to tubulin and tubulin assembly with an IC50 value of 0.85 μM, superior to the reference compound CA4 ...[more]