Folia Histochemica et Cytobiologica 2001-01-01

Cytotoxicity activity of L-proline analogues of anthraquinone-2-carboxylic acid in breast cancer MCF-7 cells.

A Bielawska, K Bielawski, J Pałka

Index: Folia Histochem. Cytobiol. 39 Suppl 2 , 207-8, (2001)

Full Text: HTML

Abstract

Although prolidase [E.C.3.4.13.9] is found in normal cells, substantially increased levels are found in some neoplastic tissues. Prolidase evokes the ability to hydrolyse the imido-bond of various low molecular weight compounds coupled to L-proline. The synthesis of three proline analogues of anthraquinone-2-carboxylic acid (1-3) has been performed. Treatment of these prodrugs with prolidase generated L-proline and the free drug, demonstrating their substrate susceptibility prolidase. The concentrations of 1, 2 and 3 needed to inhibit [1H]thymidine incorporation into DNA by 50% (IC50) in breast cancer MCF-7 cells were found to be 185 +/- 5 microM, 107 +/- 6 microM and 87 +/- 6 microM, respectively, suggesting a lower cytotoxic potency of these compounds compared to Hoechst 33228 (IC50 = 55 +/- 6 microM).

Related Compounds

  • 2-Anthraquinonecar...

Related Articles:

Detecting multiple cell-secreted cytokines from the same aptamer-functionalized electrode.

2015-02-15

[Biosens. Bioelectron. 64 , 43-50, (2014)]

Adsorption state and morphology of anthraquinone-2-carboxylic acid deposited from solution onto the atomically-smooth native oxide surface of Al(111) films studied by infrared reflection absorption spectroscopy, X-ray photoelectron spectroscopy, and atomic force microscopy.

2008-03-01

[Anal. Sci. 24(3) , 313-20, (2008)]

Prolidase as a prodrug converting enzyme. II. Synthesis of proline analogue of anthraquinone-2-carboxylic acid and its susceptibility to the action of prolidase.

[Rocz. Akad. Med. Bialymst. 43 , 201-9, (1998)]

Possible cause of G-C-->C-G transversion mutation by guanine oxidation product, imidazolone.

2001-04-01

[Chem. Biol. 8(4) , 369-78, (2001)]

Physicochemical characterization of 9,10-anthraquinone 2-carboxylic acid.

1993-12-01

[J. Pharm. Sci. 82(12) , 1250-4, (1993)]

More Articles...