Synthesis of 4-(4-methylidene-4H-3,1-benzothiazin-2-yl)benzene1,3-diols and their antiproliferative activity against human cancer cell lines
- Authors: Matysiak J.1, Skrzypek A.1, Niewiadomy A.1,2, Karpińska M.M.2, Wietrzyk J.3, Paw B.4, Kłopotowska D.3
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Affiliations:
- Department of Chemistry
- Institute of Industrial Organic Chemistry
- Department of Experimental Oncology
- Medical University of Lublin
- Issue: Vol 42, No 1 (2016)
- Pages: 93-99
- Section: Article
- URL: https://journals.rcsi.science/1068-1620/article/view/227839
- DOI: https://doi.org/10.1134/S106816201601009X
- ID: 227839
Cite item
Abstract
One-step synthesis of novel biologically active 4- or 6-(4-methylidene-4H-3,1-benzothiazin-2yl)benzene-1,3-diols is described. The target compounds were prepared by the reaction of aryl-modified sulfinylbis[(2,4-dihydroxyphenyl)methanethione]s with 1-(2-aminophenyl)ethanones. Newly synthesized compounds were characterized by IR, 1H NMR, and mass spectral data. Their antiproliferative potency against human cancer cell lines was determined. Some descriptors were calculated to find the relationship between the structure and activity. It is revealed that the presence of hydrophobic substituents in the benzenediol ring intensifies the biological potency.
About the authors
J. Matysiak
Department of Chemistry
Author for correspondence.
Email: joanna.matysiak@up.lublin.pl
Poland, Akademicka 15, Lublin, 20-950
A. Skrzypek
Department of Chemistry
Email: joanna.matysiak@up.lublin.pl
Poland, Akademicka 15, Lublin, 20-950
A. Niewiadomy
Department of Chemistry; Institute of Industrial Organic Chemistry
Email: joanna.matysiak@up.lublin.pl
Poland, Akademicka 15, Lublin, 20-950; Annopol 6, Warsaw, 03-236
M. M. Karpińska
Institute of Industrial Organic Chemistry
Email: joanna.matysiak@up.lublin.pl
Poland, Annopol 6, Warsaw, 03-236
J. Wietrzyk
Department of Experimental Oncology
Email: joanna.matysiak@up.lublin.pl
Poland, R. Weigla 12, Wroclaw, 53-114
B. Paw
Medical University of Lublin
Email: joanna.matysiak@up.lublin.pl
Poland, Jaczewskiego 4, Lublin, 20-090
D. Kłopotowska
Department of Experimental Oncology
Email: joanna.matysiak@up.lublin.pl
Poland, R. Weigla 12, Wroclaw, 53-114