Synthesis and evaluation of antifungal activity of C21-steroidal derivatives

Bioorg Med Chem Lett. 2016 Apr 15;26(8):2040-3. doi: 10.1016/j.bmcl.2016.02.080. Epub 2016 Feb 27.

Abstract

The antifungal activities of eleven C21-steroidal compounds isolated from Cynanchum wilfordii, together with thirty-six derivatives of caudatin and qingyangshengenin were evaluated on Sclerotinia sclerotiorum and other five fungal strains by the mycelium growth rate method. Four derivatives 1k, 1y, 10d, and 10j exhibited much stronger inhibitions on growth of S. sclerotiorum with IC50 values of 0.0084, 0.0049, 0.0053, and 0.0034 μM, respectively.

Keywords: Antifungal activity; C(21)-steroidal derivatives; Caudatin; Qingyangshengenin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antifungal Agents / chemical synthesis*
  • Antifungal Agents / chemistry
  • Antifungal Agents / isolation & purification
  • Antifungal Agents / pharmacology*
  • Ascomycota / drug effects*
  • Ascomycota / growth & development
  • Cynanchum / chemistry
  • Dose-Response Relationship, Drug
  • Microbial Sensitivity Tests
  • Molecular Conformation
  • Steroids / chemical synthesis
  • Steroids / chemistry
  • Steroids / isolation & purification
  • Steroids / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antifungal Agents
  • Steroids