Abstract

Lycorine, which is the most abundant alkaloid isolated from the Amaryllidaceae family of plants, reportedly exhibits promising anticancer activities. Herein, a series of novel lycorine derivatives were synthesized and evaluated for their in vitro inhibitory activities against seven different cancer cell lines, including A549, HCT116, SK-OV-3, NCI-H460, K562, MCF-7 and HL-60. The results indicated that compounds bearing diverse amine substituents at the C-2 position demonstrated good anticancer activities. The selectivity towards different cancer cell lines of the synthesized derivatives is discussed.

Highlights

  • Cancer is a proliferation disorder disease with apoptosis obstacles

  • In the present study we report the synthesis of some novel lycorine derivatives and the evaluation of their in vitro anticancer activities

  • Several derivatives were synthesized to investigate the influences of different substituents at the C-2 position

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Summary

Introduction

Cancer is a proliferation disorder disease with apoptosis obstacles. It strikes more than one-third of the World’s population and causes over 20% of all deaths [1]. The standard cancer treatment protocols include surgery, radiotherapy and chemotherapy. Chemotherapy is not effective in treating cancers associated with innate resistance to apoptosis and/or acquired resistance to drugs during treatment [2]. Discovery of novel effective anticancer medicines is of great importance. As a source of drugs, natural products play an important role in drug discovery.

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