2. Academic Validation
  3. Synthesis of novel antiproliferative hybrid bis-(3-indolyl)methane phosphonate derivatives

Synthesis of novel antiproliferative hybrid bis-(3-indolyl)methane phosphonate derivatives

  • Eur J Med Chem. 2018 Oct 5:158:874-883. doi: 10.1016/j.ejmech.2018.09.011.
Aitor Maestro,  Endika Martín-Encinas,  Concepción Alonso,  Edorta Martinez de Marigorta,  Gloria Rubiales,  Javier Vicario,  Francisco Palacios
PMID: 30253344 DOI: 10.1016/j.ejmech.2018.09.011
Abstract

An efficient synthetic methodology for the preparation of phosphorus substituted bis-(3-indolyl)methane through a double nucleophilic addition of indole derivatives to an in situ generated α-iminophosphonate is reported. In addition, bis-(3-indolyl)methane substrates showed in vitro cytotoxicity, inhibiting the growth of carcinoma human tumor cell lines A549 (carcinomic human alveolar basal epithelial cell) and SKOV03 (human ovarian carcinoma).

Keywords

Antiproliferative effect; Bis-(3-indolyl)methanes (BIMs); Indole; Phosphonate.

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