2. Academic Validation
  3. The cytotoxic properties and preferential toxicity to tumour cells displayed by some 2,4-bis(benzylidene)-8-methyl-8-azabicyclo[3.2.1] octan-3-ones and 3,5-bis(benzylidene)-1-methyl-4-piperidones

The cytotoxic properties and preferential toxicity to tumour cells displayed by some 2,4-bis(benzylidene)-8-methyl-8-azabicyclo[3.2.1] octan-3-ones and 3,5-bis(benzylidene)-1-methyl-4-piperidones

  • Eur J Med Chem. 2009 Jan;44(1):54-62. doi: 10.1016/j.ejmech.2008.03.015.
Hari N Pati 1,  Umashankar Das,  Swagatika Das,  Brian Bandy,  Erik De Clercq,  Jan Balzarini,  Masami Kawase,  Hiroshi Sakagami,  J Wilson Quail,  James P Stables,  Jonathan R Dimmock
Affiliations

Affiliation

  • 1 College of Pharmacy and Nutrition, University of Saskatchewan, 110 Science Place, Saskatoon, Saskatchewan S7N 5C9, Canada.
PMID: 18468733 DOI: 10.1016/j.ejmech.2008.03.015
Abstract

This study demonstrated that replacement of the axial protons on the C2 and C6 atoms of various 1-methyl-3,5-bis(benzylidene)-4-piperidones 3 by a dimethylene bridge leading to series 2 lowered cytotoxic potencies. Four compounds 2a and 3a-c emerged as lead molecules based on their toxicity towards different neoplasms and their selective toxicity for malignant rather than normal cells. Some possible reasons for the disparity between the IC(50) values in the two series of compounds are presented based on molecular modeling, logP values and respiration in rat liver mitochondria.

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