6E-hydroximinosteroid homodimerization by cross-metathesis processes

Steroids. 2007 Oct;72(11-12):729-35. doi: 10.1016/j.steroids.2007.03.014. Epub 2007 Apr 7.

Abstract

A rapid and efficient synthesis of 6E-hydroximinosteroid homodimers is described. The two new compounds were linked at position 3 of the steroid nucleus via a ruthenium catalyzed cross-metathesis reaction. The cytotoxic activity of these compounds was evaluated in vitro on human lung carcinoma A549 (ATCC CCL-185), colon adenocarcinoma HCT-116 (ATCC CCL-247), human caucasian glioblastoma multiforme T98G (ECACC 92090213) and human pancreatic adenocarcinoma PSN1 (ECACC 94060601) tumour cells. Homodimer 10b presented selective activity against HCT-116, although they are not highly toxic when compared with the monomer counterparts.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Death / drug effects
  • Cell Line, Tumor
  • Chemistry, Organic / methods*
  • Dimerization
  • Drug Screening Assays, Antitumor
  • Humans
  • Inhibitory Concentration 50
  • Steroids / chemical synthesis*
  • Steroids / chemistry
  • Steroids / pharmacology

Substances

  • 6E-hydroximinosteroid
  • Steroids