Synthesis and biological activity of salinomycin-hydroxamic acid conjugates

Bioorg Med Chem Lett. 2017 Apr 1;27(7):1624-1626. doi: 10.1016/j.bmcl.2017.01.080. Epub 2017 Jan 28.

Abstract

Several salinomycin-hydroxamic acid conjugates were designed and synthesized. Most conjugates showed better antiproliferative activities than salinomycin in HT-29 colon cancer, HGC-27 gastric cancer, and especially in MDA-MB-231 triple-negative human breast cancer cells. These conjugates are stable in cell culture media, and they showed much better biological activities than the 1:1 physical mixture with hydroxamic acids and salinomycin. The better membrane permeability and hydrolysis rate of the conjugates may lead to the activity improvements.

Keywords: Anti-cancer; Conjugates; Hydroxamic acid; Salinomycin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Drug Stability
  • Humans
  • Hydroxamic Acids / chemical synthesis
  • Hydroxamic Acids / pharmacology*
  • Pyrans / chemical synthesis
  • Pyrans / pharmacology*

Substances

  • Antineoplastic Agents
  • Hydroxamic Acids
  • Pyrans
  • salinomycin