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Synthesis and the Biological Activity of Phosphonylated 1,2,3-Triazolenaphthalimide Conjugates.

Synthesis and the Biological Activity of Phosphonylated 1,2,3-Triazolenaphthalimide Conjugates.
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Głowacka IE, Gulej R, Grzonkowski P, Andrei G, Schols D, Snoeck R, Piotrowska DG,


Głowacka IE, Gulej R, Grzonkowski P, Andrei G, Schols D, Snoeck R, Piotrowska DG, (click to view)

Głowacka IE, Gulej R, Grzonkowski P, Andrei G, Schols D, Snoeck R, Piotrowska DG,

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Molecules (Basel, Switzerland) 2016 Oct 2621(11) pii E1420
Abstract

A novel series of diethyl {4-[(5-substituted-1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl)-methyl]-1H-1,2,3-triazol-1-yl}alkylphosphonates designed as analogues of amonafide was synthesized. All phosphonates were assessed for antiviral activity against a broad range of DNA and RNA viruses and several of them showed potency against varicella-zoster virus (VZV) [EC50 (50% effective concentration) = 27.6-91.5 μM]. Compound 16b exhibited the highest activity against a thymidine kinase-deficient (TK(-)) VZV strain (EC50 = 27.59 μM), while 16d was the most potent towards TK⁺ VZV (EC50 = 29.91 μM). Cytostatic properties of the compounds 14a-i-17a-i were studied on L1210, CEM, HeLa and HMEC-1 cell lines and most of them were slightly cytostatic for HeLa [IC50 (50% inhibitory concentration) = 29-130 µM] and L1210 cells [IC50 (50% inhibitory concentration) = 14-142 µM].

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