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Molecules 2014, 19(8), 11300-11315; doi:10.3390/molecules190811300

Semi-Automatic Synthesis, Antiproliferative Activity and DNA-Binding Properties of New Netropsin and bis-Netropsin Analogues

1
Saint Brunon Farmacy, Bohaterów Westerplatte 4 Str., 11-500 Giżycko, Poland
2
Department of Organic Chemistry, Medical University, Mickiewicza 2A Str., 15-222 Białystok, Poland
In 2006 last name was changed from Bartulewicz.
*
Author to whom correspondence should be addressed.
Received: 17 April 2014 / Revised: 15 July 2014 / Accepted: 16 July 2014 / Published: 31 July 2014
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [799 KB, uploaded 31 July 2014]   |  

Abstract

A general route for the semi-automatic synthesis of some new potential minor groove binders was established. Six four-numbered sub-libraries of new netropsin and bis-netropsin analogues have been synthesized using a Syncore Reactor. The structures of the all new substances prepared in this investigation were fully characterized by NMR (1H, 13C), HPLC and LC-MS. The antiproliferative activity of the obtained compounds was tested on MCF-7 breast cancer cells. The ethidium displacement assay using pBR322 confirmed the DNA-binding properties of the new analogues of netropsin and bis-netropsin. View Full-Text
Keywords: combinatorial chemistry; solid phase synthesis; netropsin analogue; non-intercalative DNA binding agent; DNA minor groove binder combinatorial chemistry; solid phase synthesis; netropsin analogue; non-intercalative DNA binding agent; DNA minor groove binder
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This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Szerszenowicz, J.; Drozdowska, D. Semi-Automatic Synthesis, Antiproliferative Activity and DNA-Binding Properties of New Netropsin and bis-Netropsin Analogues. Molecules 2014, 19, 11300-11315.

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