Auspicious role of the steroidal heterocyclic derivatives as a platform for anti-cancer drugs

Bioorg Chem. 2017 Aug:73:128-146. doi: 10.1016/j.bioorg.2017.06.006. Epub 2017 Jun 20.

Abstract

Steroids are polycyclic compounds that have a wide range of biological activities. They are bio-synthesized from cholesterol through a series of enzyme-mediated transformations, so they are highly lipophilic and readily enter most cells to interact with intracellular receptors, making them ideal vehicles for targeting a broad array of pathologies. New curative agents for cancers have been developed from several steroidal derivatives. Some biologically important properties of modified steroids are dependent on structural features of the steroid moiety and their side chains. Therefore, chemical derivatization of steroids provides a way to modify their function, and many structure-activity relationships have been confirmed by such synthetic modifications. Several studies demonstrate that steroidal heterocyclic derivatives can be effective in the prevention and treatment of many types of hormone-dependent cancers. The present review is a concise report on steroidal heterocyclic derivatives, with special emphasis on steroid heterocyclic derivatives with 5 membered rings or six-membered rings having interesting therapeutic potential as enzyme inhibitors and cytotoxic drugs to be used as candidates for anti-cancer drug development.

Keywords: Anti-cancer; Five-membered rings; Heterocyclic compounds; Six-membered rings; Steroids.

Publication types

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

MeSH terms

  • Animals
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Proliferation / drug effects
  • Drug Screening Assays, Antitumor
  • Humans
  • Molecular Conformation
  • Steroids, Heterocyclic / chemical synthesis
  • Steroids, Heterocyclic / chemistry
  • Steroids, Heterocyclic / pharmacology*

Substances

  • Antineoplastic Agents
  • Steroids, Heterocyclic