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2005-04-01 - Article/Dans un journal avec peer-review - Anglais - 15 page(s)

Vanden Eynde Jean-Jacques , Mayence A., Johnson M.T., Huang T.L., Collins M.S., Walzer P.D., Cushion M.T., Donkor I.O., "Antitumor and Anti-Pneumocystis carinii Activities of Novel Bisbenzamidines" in Medicinal Chemistry Research : An International Journal for Rapid Communications on Design and Mechanisms of Action of Biologically Active Agents, 14, 3, 143 - 157

  • Edition : Birkha¨user, Boston (MA)
  • Codes CREF : Chimie organique (DI1313)
  • Unités de recherche UMONS : Chimie organique (S836)
Texte intégral :

Abstract(s) :

(Anglais) Among a library of 17 bisbenzamidines connected with various linkers, compounds with a flexible pentanediamide (10) or hexanediamide (12) linker were the most potent derivatives against rat Pneumocystis carinii (IC50 values of 3 and 2 nM, respectively) and had the highest selectivity index ratios (GI50 of human tumor cells/IC50 of rat P. carinii cells) of >104. Seven compounds caused 50% growth inhibition (GI50) of tumor cells at concentrations of <100 µM while the remaining ten were not cytotoxic. DNA binding affinity (?Tm) of the tested compounds did not correlate with either their anti-P. carinii activity or cytotoxicity.

Notes :
  • (Anglais) Lecture en ligne: http://www.springerlink.com/content/577485848h63061n/fulltext.pdf
Identifiants :
  • DOI : 10.1007/s00044-005-0130-2