Abstract
Piperlongumine is a natural amide alkaloid isolated from several species of Piper and is described in the literature as selectively cytotoxic to several cancer cell lines. Inhibiting cell migration has gained considerable interest as an approach for discovering antimetastatic agents because this process is fundamental to metastasis. Piperlongumine, selected from cell-based assay screening of NuBBE Database, inhibited the migration of MDA-MB-231 breast cancer cells with an EC50 of 3.0 ± 1.0 µM by the Boyden chamber assay. A series of five analogous compounds based on the structure of piperlongumine were designed, synthesized and evaluated in cell migration and cytotoxicity assays. The analogue designed by molecular simplification ((E)-N-acryloyl-3-(3,4,5-trimethoxyphenyl)acrylamide) was the most active of the series, with an EC50 of 1.5 ± 1 µM. Additionally, this compound was selectively cytotoxic, with a selectivity index (SI) of 4.4.
Highlights
Metastasis is the process by which undifferentiated cancer cells migrate to other parts of the body.[1,2] Suppression of metastasis is an urgent need in cancer treatment, as most existing drugs only inhibit cell proliferation.[3]
Piperlongumine, which was selected among many natural compounds already identified and available in NuBBEDB, inhibited migration of the breast cancer cell line MDA‐MB-231 with an EC50 of 3 ± 1 μM by the Boyden chamber assay
5 was the most active, with an EC50 of 1.5 ± 1 μM against breast cancer cell MDA-MB-231 migration by the Boyden chamber assay
Summary
Metastasis is the process by which undifferentiated cancer cells migrate to other parts of the body.[1,2] Suppression of metastasis is an urgent need in cancer treatment, as most existing drugs only inhibit cell proliferation.[3]. The Boyden chamber assay employs a two-compartment system separated by a membrane to quantitatively evaluate the effect of compounds on the migration of cancer cells in vitro.[28,30]
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