Synthesis and cytotoxicity testing of new amido-substituted triazolopyrrolo[2,1-c][1,4]benzodiazepine (PBDT) derivatives

Molecules. 2012 Jul 25;17(8):8762-72. doi: 10.3390/molecules17088762.

Abstract

A series of amido-substituted triazolopyrrolo[2,1-c][1,4]benzodiazepine (PBDT) derivatives was synthesized from isatoic anhydride, and their cytotoxicity against the MRC-5 and Mahlavu cell lines was evaluated. The results suggest that compound PBDT-7i with the meta-trifluoromethylbenzoyl substituent can selectively inhibit the growth of Mahlavu cells and has low toxicity towards MRC-5 cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / toxicity
  • Benzodiazepines / chemical synthesis*
  • Benzodiazepines / pharmacology
  • Benzodiazepines / toxicity
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Drug Screening Assays, Antitumor
  • Fibroblasts / drug effects
  • Fibroblasts / metabolism
  • Fibroblasts / physiology
  • Humans
  • Pyrroles / chemical synthesis*
  • Pyrroles / pharmacology
  • Pyrroles / toxicity
  • Sincalide / metabolism
  • Triazoles / chemical synthesis*
  • Triazoles / pharmacology
  • Triazoles / toxicity

Substances

  • Antineoplastic Agents
  • Pyrroles
  • Triazoles
  • Benzodiazepines
  • Sincalide