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Anticancer properties of bisaminoquinolines with modified linkers
Yuanhao Wang1, Vaibhav Jain2, Amanda Versace2
1Department of Chemistry, University of Pennsylvania, United States.
Abstract:
We have previously reported the unique features of dimeric bisaminoquinolines as anticancer agents and have identified their cellular target as PPT1, a protein palmitoyl-thioesterase. We now report a systematic study on the role of the linker in these constructs, both with respect to the distance between the heterocycles, the linker hydrophobicity and the methylation status (primary vs. secondary vs. tertiary) of the central nitrogen atom on the observed biological activity.
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