Synthesis and Antitumor Evaluation of Novel Cyclic Arylsulfonylureas: ADME-T and Pharmacophore Prediction

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Title Synthesis and Antitumor Evaluation of Novel Cyclic Arylsulfonylureas: ADME-T and Pharmacophore Prediction
Author El-Deeb, Ibrahim Mustafa; Bayoumi, Said M.; El-Sherbeny, Magda A.; Abdel-Aziz, Alaa A.-M.
Journal Name European Journal of Medicinal Chemistry
Year Published 2010
Place of publication France
Publisher Elsevier France
Abstract Novel derivatives of 5-(substituted)benzylidene-3-(4-substituted)phenylsulfonylimidazolidine-2,4-diones (3a–r), 1-(4-substituted)phenylsulfonyl-3-(4-substituted)phenylpyrimidine-2,4,6-(1H,3H,5H)-triones (6a–l), and 3-(4-substituted)phenyl-1-(4-substituted)phenylsulfonylquinazoline-2,4(1H,3H)- diones (8a–l) have been synthesized and tested for their antitumor activity against 60 tumor cell lines taken from 9 different organs. The tested compounds have showed good inhibitory effect at the ovarian cancer (IGROV1) cell line. A significant inhibition for (RXF393) renal cancer cells was observed with series 3 compounds, while in the other two series 6 and 8, there was a significant inhibition of ovarian cancer cells (OVCAR-8) and melanoma cells (SK-MEL-2). Interestingly; beside the strong inhibition of compound 3q to IGROV1 and RXF393 cells, a great inhibition (199.62%) for (M14) Melanoma cells was observed at the tested concentration (10 μM). ADME-T and pharmacophore prediction methodology were used to study the antitumor activity of the most active compounds and to identify the structural features required for antitumor activity.
Peer Reviewed Yes
Published Yes
Alternative URI http://dx.doi.org/10.1016/j.ejmech.2010.02.038
Copyright Statement Copyright 2010 Elsevier Inc. This is the author-manuscript version of this paper. Reproduced in accordance with the copyright policy of the publisher. Please refer to the journal's website for access to the definitive, published version.
Volume 45
Issue Number 6
Page from 2516
Page to 2530
ISSN 0223-5234
Date Accessioned 2011-03-18
Date Available 2011-07-20T07:06:41Z
Language en_AU
Research Centre Institute for Glycomics
Faculty Faculty of Science, Environment, Engineering and Technology
Subject Biologically Active Molecules
URI http://hdl.handle.net/10072/37838
Publication Type Journal Articles (Refereed Article)
Publication Type Code c1x

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