Silicon-containing analogs of camptothecin as anticancer agents

Arch Pharm (Weinheim). 2018 Jan;351(1). doi: 10.1002/ardp.201700297. Epub 2017 Dec 14.

Abstract

The plant pentacyclic alkaloid camptothecin and its structural analogs were extensively studied. These compounds are interesting due to the antitumor activity associated with their ability to inhibit topoisomerase I in tumor cells. During the last decades of the 20th century, a large number of the silicon-containing camptothecins (silatecans) were synthesized. 7-tert-Butyldimethylsilyl-10-hydroxy-camptothecin (DB-67 or AR-67) has enhanced lipophilicity and demonstrates a antitumor activity superior to its carbon analog. To date, certain silatecans are under clinical trials and their ultimate role in cancer therapy appears promising. In this review, we present chemical methodologies for the synthesis of silicon-containing camptothecins, their chemical properties, biological activity, and results of clinical trials.

Keywords: biological activity; camptothecin; properties; silatecans; synthesis.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents, Phytogenic / chemistry
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Camptothecin / chemistry
  • Camptothecin / pharmacology*
  • Cell Proliferation / drug effects
  • Humans
  • Molecular Structure
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Silicon / chemistry
  • Silicon / pharmacology*

Substances

  • Antineoplastic Agents, Phytogenic
  • Camptothecin
  • Silicon