Apoptosis inducing properties of 3-biotinylate-6-benzimidazole B-nor-cholesterol analogues

Steroids. 2021 May:169:108822. doi: 10.1016/j.steroids.2021.108822. Epub 2021 Mar 12.

Abstract

In this work, a series of Biotin-substituted B-nor-cholesteryl benzimidazole compounds were synthesized. The antiproliferativeactivities of these compounds were evaluated in vitro using a series of human cancer cell lines, including HeLa (cervical cancer), SKOV3 (ovarian cancer), T-47D (thymus gland cancer), MCF-7 (human breast cancer) and HEK293T (normal renal epithelial) cells. These compounds displayed distinct antiproliferative activities against the currently tested cancer cells. The apoptotic properties induced by compound 6d were further investigated. Our results showed that compound 6d could induce the apoptosis of SKOV3 cells, blocking the cell growth in S-phase. Western blotting analyses revealed that compound 6d can induce cell apoptosis via the mitochondria-dependent pathway.

Keywords: Apoptosis; B-nor-cholesterol; Benzimidazole; Cell-cycle; Synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Apoptosis / drug effects
  • Benzimidazoles*
  • Cell Cycle / drug effects
  • Cell Proliferation / drug effects
  • HEK293 Cells
  • Humans
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Benzimidazoles
  • benzimidazole