Anticancer properties of bisaminoquinolines with modified linkers

Bioorg Med Chem Lett. 2021 Oct 1:49:128272. doi: 10.1016/j.bmcl.2021.128272.

Yuanhao Wang ¹, Vaibhav Jain ², Amanda Versace ², Monika Bhardwaj ², Mary Ann S Crissey ², Ravi K Amaravadi ³, Jeffrey D Winkler ⁴

Affiliations

1 Department of Chemistry, University of Pennsylvania, United States.
2 Department of Medicine and Abramson Cancer Center, University of Pennsylvania, United States.
3 Department of Medicine and Abramson Cancer Center, University of Pennsylvania, United States. Electronic address: ravi.amaravadi@pennmedicine.upenn.edu.
4 Department of Chemistry, University of Pennsylvania, United States. Electronic address: winkler@sas.upenn.edu.

PMID: 34298133 DOI: 10.1016/j.bmcl.2021.128272

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.

Keywords

Anticancer; Autophagy; Dimer; Quinoline.

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