Molecules 2017, 22(5), 794; https://doi.org/10.3390/molecules22050794
Synthesis, Biological Activity and Preliminary in Silico ADMET Screening of Polyamine Conjugates with Bicyclic Systems
Marta Szumilak 1
, Malgorzata Galdyszynska 2, Kamila Dominska 2, Irena I. Bak-Sypien 3, Anna Merecz-Sadowska 3, Andrzej Stanczak 1, Boleslaw T. Karwowski 3,*
and Agnieszka W. Piastowska-Ciesielska 2,4
, Malgorzata Galdyszynska 2, Kamila Dominska 2, Irena I. Bak-Sypien 3, Anna Merecz-Sadowska 3, Andrzej Stanczak 1, Boleslaw T. Karwowski 3,*
and Agnieszka W. Piastowska-Ciesielska 2,41
Department of Hospital Pharmacy, Faculty of Pharmacy, Medical University of Lodz, 1 Muszynskiego Street, 90-151 Lodz, Poland
2
Department of Comparative Endocrinology, Medical University of Lodz, 7/9 Zeligowskiego Street, 90-752 Lodz, Poland
3
Food Science Department, Faculty of Pharmacy, Medical University of Lodz, 1 Muszynskiego Street, 90-151 Lodz, Poland
4
Laboratory of Cell Cultures and Genomic Analysis, Medical University of Lodz, 7/9 Zeligowskiego Street, Lodz 90-752, Poland
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 20 March 2017 / Revised: 28 April 2017 / Accepted: 9 May 2017 / Published: 12 May 2017
(This article belongs to the Special Issue Nucleic Acid Chemistry and Nucleic Acid Drugs: A Themed Issue in Honor of Professor Lihe Zhang on the Occasion of His 80th Birthday)
Abstract
Polyamine conjugates with bicyclic terminal groups including quinazoline, naphthalene, quinoline, coumarine and indole have been obtained and their cytotoxic activity against PC–3, DU–145 and MCF–7 cell lines was evaluated in vitro. Their antiproliferative potential differed markedly and depended on both their chemical structure and the type of cancer cell line. Noncovalent DNA-binding properties of the most active compounds have been examined using ds–DNA thermal melting studies and topo I activity assay. The promising biological activity, DNA intercalative binding mode and favorable drug-like properties of bis(naphthalene-2-carboxamides) make them a good lead for further development of potential anticancer drugs. View Full-Text
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Szumilak, M.; Galdyszynska, M.; Dominska, K.; Bak-Sypien, I.I.; Merecz-Sadowska, A.; Stanczak, A.; Karwowski, B.T.; Piastowska-Ciesielska, A.W. Synthesis, Biological Activity and Preliminary in Silico ADMET Screening of Polyamine Conjugates with Bicyclic Systems. Molecules 2017, 22, 794.
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