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Issue 63, 2019
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Structure–activity–distribution relationship study of anti-cancer antimycin-type depsipeptides

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Abstract

Small-molecule natural products have been an essential source of pharmaceuticals to treat human diseases, but very little is known about their behavior inside dynamic, live human cells. Here, we demonstrate the first structure–activity–distribution relationship (SADR) study of complex natural products, the anti-cancer antimycin-type depsipeptides, using the emerging bioorthogonal Stimulated Raman Scattering (SRS) Microscopy. Our results show that the intracellular enrichment and distribution of these compounds are driven by their potency and specific protein targets, as well as the lipophilic nature of compounds.

Graphical abstract: Structure–activity–distribution relationship study of anti-cancer antimycin-type depsipeptides

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Supplementary files

Article information


Submitted
19 Apr 2019
Accepted
11 Jul 2019
First published
16 Jul 2019

Chem. Commun., 2019,55, 9379-9382
Article type
Communication
Author version available

Structure–activity–distribution relationship study of anti-cancer antimycin-type depsipeptides

J. Seidel, Y. Miao, W. Porterfield, W. Cai, X. Zhu, S. Kim, F. Hu, S. Bhattarai-Kline, W. Min and W. Zhang, Chem. Commun., 2019, 55, 9379
DOI: 10.1039/C9CC03051D

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