Synthesis of oleandrin derivatives and their cytotoxic activity.

Steroids

Shanghai Research Center for Modernization of Traditional Chinese Medicine, National Engineering Laboratory for TCM Standardization Technology, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China; University of Chinese Academy of Sciences, Beijing 100049, PR China. Electronic address:

Published: July 2020

AI Article Synopsis

  • A series of oleandrin-4'-yl ester derivatives were created to test their effects on tumor cell growth.
  • The study found that the specific structure of the C4' part of these compounds significantly influenced their ability to kill cancer cells.
  • The compound 4b-HCl showed promising results, significantly reducing tumor growth by 96.4% at a low dose and having good water solubility for potential medical use.*

Article Abstract

A series of oleandrin-4'-yl ester derivatives were designed, synthesized, and evaluated for their proliferation inhibition activities against tumor cell lines. Cytotoxicity data revealed that the C4' moiety had an important influence on cytotoxic activity. Several compounds that we designed and synthesized exhibit significant in vitro antiproliferative activity against the tested tumor cell lines. Among the derivatives of OL, 4b-HCl not only had good anti-tumor activity but also had good water solubility. Furthermore, 4b-HCl can significantly inhibit tumor growth by 96.4% at a dose of 6 mg/kg/d by ip.

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http://dx.doi.org/10.1016/j.steroids.2020.108650DOI Listing

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