Norcantharidin analogues — Synthesis and evaluation of growth inhibition in a panel of selected tumor-cell lines

Authors: Deng, Liping; Shen, Li; Zhang, Jing; Yang, Bo; He, Qiaojun; Hu, Yongzhou

Source: Canadian Journal of Chemistry, Volume 85, Number 11, November 2007 , pp. 938-944(7)

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Abstract:

A series of norcantharidin (NCTD) analogues have been synthesized by [3+2]1,3-dipolar cycloaddition reaction of norcantharidin derivatives of substituted aromatic amines with four nitrile oximes. All analogues have been screened for their antiproliferative activity in vitro against a panel of tumor cell lines: KB, SGC-7901, HL60, Bel-7402, HO-8910, and ECA109, producing IC₅₀ values from 0.36 µmol/L to >100 µmol/L. Compound 9d showed potency for the treatment of hepatoma, with IC₅₀ value to Bel-7402 cell line comparable to that of norcantharidin.Key words: norcantharidin analogues, isoxazoline, growth inhibition.

On a réalisé la synthèse d'une série d'analogues de la norcantharidine en procédant à une réaction de cycloaddition 1,3-dipolaire [3+2] de dérivés de la norcantharidine d'amines aromatiques substituées avec quatre oximes de nitriles. On a évalué l'activité comme inhibiteur de croissance in vitro de chacun des analogues contre un ensemble de souches de cellules tumorales: KB, SGC-7901, HL60, Bel-7402, HO-8910 et ECA109 pour lesquelles les valeurs de IC₅₀ varient de 0,36 µmol/L à plus de 100 µmol/L. Le composé 9d présente un grand potentiel pour le traitement de l'hépatome, avec une valeur de IC₅₀ qui, par comparaison avec celle des cellules Bel-7402, est comparable à celle de la norcantharidine.Mots-clés : analogues de la norcantharidine, isoxazoline, inhibition de la croissance. [Traduit par la Rédaction]

Document Type: Research article

Publication date: 2007-11-01

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Norcantharidin analogues — Synthesis and evaluation of growth inhibition in a panel of selected tumor-cell lines

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