Synthesis and Antiproliferative Activity of Silybin Conjugates with Salinomycin and Monensin

Chem Biol Drug Des. 2015 Dec;86(6):1378-86. doi: 10.1111/cbdd.12602. Epub 2015 Jul 22.

Abstract

Aiming at development of multitarget drugs for the anticancer treatment, new silybin (SIL) conjugates with salinomycin (SAL) and monensin (MON) were synthesized, in mild esterification conditions, and their antiproliferative activity was studied. The conjugates obtained exhibit anticancer activity against HepG2, LoVo and LoVo/DX cancer cell lines. Moreover, MON-SIL conjugate exhibits higher anticancer potential and better selectivity than the corresponding SAL-SIL conjugate.

Keywords: anticancer activity; molecular hybrids; natural products; polyether antibiotics; silibinin.

Publication types

  • Letter
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • BALB 3T3 Cells
  • Cell Line, Tumor
  • Cell Proliferation / drug effects*
  • Drug Design
  • Drug Screening Assays, Antitumor
  • Hep G2 Cells
  • Humans
  • Mice
  • Monensin / chemical synthesis
  • Monensin / chemistry
  • Monensin / pharmacology*
  • Pyrans / chemical synthesis
  • Pyrans / chemistry
  • Pyrans / pharmacology*
  • Silybin
  • Silymarin / chemical synthesis
  • Silymarin / chemistry
  • Silymarin / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Pyrans
  • Silymarin
  • Silybin
  • salinomycin
  • Monensin