1. Academic Validation
  2. Asymmetrical 2,6-bis(benzylidene)cyclohexanones: Synthesis, cytotoxic activity and QSAR study

Asymmetrical 2,6-bis(benzylidene)cyclohexanones: Synthesis, cytotoxic activity and QSAR study

  • Eur J Med Chem. 2012 Apr:50:113-23. doi: 10.1016/j.ejmech.2012.01.045.
Maryam Nakhjiri 1 Maliheh Safavi Eskandar Alipour Saeed Emami Amir Farzin Atash Mona Jafari-Zavareh Sussan K Ardestani Mehdi Khoshneviszadeh Alireza Foroumadi Abbas Shafiee
Affiliations

Affiliation

  • 1 Drug Design & Development Research Center, Tehran University of Medical Sciences, Tehran, Iran.
Abstract

In order to develop novel anti-cancer agents, a series of asymmetrical 2,6-bis (benzylidene)cyclohexanone derivatives containing nitrobenzylidene moiety were synthesized and their cytotoxic activity were determined in vitro against MDA-MB 231, MCF-7 and SK-N-MC cell lines using MTT assay. Among the tested compounds, the highest activity against MDA-MB 231 cells was achieved by 2-(3-bromo-5-methoxy-4-propoxybenzylidene)-6-(2-nitrobenzylidene)cyclohexanone (compound 5d). Whereas, compound 5j (the 3-nitro analog of compound 5d) was the most potent compound against MCF-7 and SK-N-MC cell lines. The results indicated that the cytotoxic activity profile against different tumor cells can be optimized by desired 4-alkoxy-3-bromo-5-methoxybenzylidene scaffold.

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