Chalcone-benzoxaborole hybrids as novel anticancer agents

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5797-5801. doi: 10.1016/j.bmcl.2016.10.024. Epub 2016 Oct 12.

Abstract

In this study, we report the synthesis of a series of chalcone-benzoxaborole hybrid molecules and the evaluation of their anticancer activity. Their anticancer potency and toxicity were tested on three human cancer cell lines and two normal cell lines. The 4-fluoro compound 15 was found to be the most potent compound with an IC50 value of 1.4μM on SKOV3 cells. The 4-iodo compound 18 and 3-methyloxy-4-amino compound 47 showed good potency on SKOV3 cells while exhibiting low toxicity on normal cells. This work extended the application of benzoxaboroles to the field of anticancer research.

Keywords: Anticancer; Benzoxaborole; Drug discovery; Structure–activity relationship.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology*
  • Boron Compounds / chemistry*
  • Boron Compounds / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Chalcone / analogs & derivatives*
  • Chalcone / pharmacology*
  • Drug Discovery
  • Drug Screening Assays, Antitumor
  • Humans
  • Neoplasms / drug therapy
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Boron Compounds
  • Chalcone