Structural factors affecting cytotoxic activity of (E)-1-(Benzo[d ][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one derivatives.

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ID: 3617
2014
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Abstract
Derivatives of (E)-1-(5-alkoxybenzo[d][1,3]oxathiol-6-yl)-3-phenylprop-2-en-1-one demonstrated exceptionally high in vitro cytotoxic activity, with IC50 values of the most active derivatives in the nanomolar range. To identify structural fragments necessary for the activity, several analogs deprived of selected fragments were prepared, and their cytotoxic activity was tested. It was found that the activity depends on combined effects of (i) the heterocyclic ring, (ii) the alkoxy group at position 5 of the benzoxathiole ring, and (iii) the substituents in the phenyl ring B. Replacement of the sulfur atom by oxygen does not influence the activity. None of the listed structural fragments alone assured high cytotoxic activity.
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konieczny2014structuralchemical Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Konieczny, Marek T;Bułakowska, Anita;Polak, Justyna;Pirska, Danuta;Konieczny, Wojciech;Gryń, Patrycja;Skladanowski, Andrzej;Sabisz, Michał;Lemke, Krzysztof;Pieczykolan, Anna;Gałązka, Marlena;Wiciejowska, Katarzyna;Wietrzyk, Joanna;
Journal Chemical biology & drug design
Year 2014
DOI
10.1111/cbdd.12296
URL
Keywords Keywords not found

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