Steroidal derivatives. Part 1: some novel steroidal thiosemicarbazones. Their synthesis, anticancer and endocrinological activities

Pharmazie. 1978 Sep;33(9):577-80.

Abstract

The synthesis of several novel thiosemicarbazone derivatives of steroids, including estrogens and androgens, is described. Evaluation of the products in P 388 Lymphocytic Leukemia indicated no anticancer activity. The endocrinological screening showed that estrogenicity is slightly reduced but not abolished in the thiosemicarbazones derived from estrone-3-methyl ether (compounds 1, 2 and 4). The androgenic activity of the thiosemicarbazones derived from testosterone (compounds 7--9) was more pronounced than that of testosterone. Among the same thiosemicarbazone derivatives 7--9, only o-tolyl derivative 8 exhibited anabolic activity.

MeSH terms

  • Animals
  • Antineoplastic Agents
  • Estradiol / pharmacology
  • Female
  • Male
  • Mice
  • Muscles / drug effects
  • Organ Size / drug effects
  • Prostate / drug effects
  • Rats
  • Steroids / chemical synthesis*
  • Steroids / pharmacology
  • Testosterone / pharmacology
  • Thiosemicarbazones / chemical synthesis*
  • Thiosemicarbazones / pharmacology
  • Uterus / drug effects

Substances

  • Antineoplastic Agents
  • Steroids
  • Thiosemicarbazones
  • Testosterone
  • Estradiol