Issue 45, 2020

Systematically altering the lipophilicity of rhenium(i) tricarbonyl anticancer agents to tune the rate at which they induce cell death

Abstract

Rhenium-based anticancer agents have arisen as promising alternatives to conventional platinum-based drugs. Based on previous studies demonstrating how increasing lipophilicity improves drug uptake within the cell, we sought to investigate the effects of lipophilicity on the anticancer activity of a series of six rhenium(I) tricarbonyl complexes. These six rhenium(I) tricarbonyl structures, called Re-Chains, bear pyridyl imine ligands with different alkyl chains ranging in length from two to twelve carbons. The cytotoxicities of these compounds were measured in HeLa cells. At long timepoints (48 h), all compounds are equally cytotoxic. At shorter time points, however, the compounds with longer alkyl chains are significantly more active than those with smaller chains. Cellular uptake studies of these compounds show that they are taken up via both passive and active pathways. Collectively, these studies show how lipophilicity affects the rate at which these Re compounds induce their biological activities.

Graphical abstract: Systematically altering the lipophilicity of rhenium(i) tricarbonyl anticancer agents to tune the rate at which they induce cell death

Supplementary files

Article information

Article type
Communication
Submitted
23 Cig 2020
Accepted
11 Agd 2020
First published
22 Agd 2020

Dalton Trans., 2020,49, 16062-16066

Author version available

Systematically altering the lipophilicity of rhenium(I) tricarbonyl anticancer agents to tune the rate at which they induce cell death

C. C. Konkankit, B. A. Vaughn, Z. Huang, E. Boros and J. J. Wilson, Dalton Trans., 2020, 49, 16062 DOI: 10.1039/D0DT01097A

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements