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. 2017 Jan 5:125:453-463.
doi: 10.1016/j.ejmech.2016.09.048. Epub 2016 Sep 16.

Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents (V体育安卓版)

Mary J Meegan  1 , Seema Nathwani  2 , Brendan Twamley  3 , Daniela M Zisterer  2 , Niamh M O'Boyle  4
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Piperlongumine (piplartine) and analogues: Antiproliferative microtubule-destabilising agents

"V体育官网" Mary J Meegan et al. Eur J Med Chem. .

Abstract

Piperlongumine (piplartine, 1) is a small molecule alkaloid that is receiving intense interest due to its antiproliferative and anticancer activities. We investigated the effects of 1 on tubulin and microtubules. Using both an isolated tubulin assay, and a combination of sedimentation and western blotting, we demonstrated that 1 is a tubulin-destabilising agent. This result was confirmed by immunofluorescence and confocal microscopy, which showed that microtubules in MCF-7 breast cancer cells were depolymerized when treated with 1. We synthesised a number of analogues of 1 to explore structure-activity relationships. Compound 13 had the best cytotoxic profile of this series, showing potent effects in human breast carcinoma MCF-7 cells whilst being relatively non-toxic to non-tumorigenic MCF-10a cells VSports手机版. These compounds will be further developed as potential clinical candidates for the treatment of breast cancer. .

Keywords: Anticancer; Antiproliferative; Combretastatin A-4; Microtubule-destabilising; Piperlongumine; Tubulin. V体育安卓版.

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