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 ( …

…, B Bandy, E De Clercq, J Balzarini, M Kawase…

Index: Pati, Hari N.; Das, Umashankar; Das, Swagatika; Bandy, Brian; De Clercq, Erik; Balzarini, Jan; Kawase, Masami; Sakagami, Hiroshi; Quail, J. Wilson; Stables, James P.; Dimmock, Jonathan R. European Journal of Medicinal Chemistry, 2009 , vol. 44, # 1 p. 54 - 62

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Citation Number: 50

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 ...