Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Selective Interactions with Various G-Quadruplex DNA Forming Sequences by Berberine and Palmatine Analogues

Marco Franceschin
* ,
Lorenzo Cianni
,
Massimo Pitorri
,
Emanuela Micheli
,
Stefano Cacchione
,
Claudio Frezza
* ORCID logo ,
Mauro Serafini
,
Minghou Hu
,
Huafi Su
,
Zhishu Huang
,
Lianquan Gu
,
Armandodoriano Bianco
ORCID logo
Version 1 : Received: 12 May 2018 / Approved: 14 May 2018 / Online: 14 May 2018 (11:44:10 CEST)

A peer-reviewed article of this Preprint also exists.

Franceschin, M.; Cianni, L.; Pitorri, M.; Micheli, E.; Cacchione, S.; Frezza, C.; Serafini, M.; Hu, M.-H.; Su, H.; Huang, Z.; Gu, L.; Bianco, A. Natural Aromatic Compounds as Scaffolds to Develop Selective G-Quadruplex Ligands: From Previously Reported Berberine Derivatives to New Palmatine Analogues. Molecules 2018, 23, 1423. Franceschin, M.; Cianni, L.; Pitorri, M.; Micheli, E.; Cacchione, S.; Frezza, C.; Serafini, M.; Hu, M.-H.; Su, H.; Huang, Z.; Gu, L.; Bianco, A. Natural Aromatic Compounds as Scaffolds to Develop Selective G-Quadruplex Ligands: From Previously Reported Berberine Derivatives to New Palmatine Analogues. Molecules 2018, 23, 1423.

Abstract

In this article/review, the selective interactions of several berberine and palmatine derivatives with various DNA G-quadruplex structures are reported. These derivatives were constructed starting from two natural compounds, berberine and palamatine, through specific synthetic passages following two different schemes for each of them and using several substituents. The details of these synthesis are also described. Indeed, the study of the interactions of these derivative compounds with various G-quadruplex forming sequences was carried out by means of various structural and biochemical techniques. The results show that the presence of suitable side chains are very useful to improve the interaction of the ligands with G-quadruplex structures. Thus, since G-quadruplex formation is promoted by these compounds, which have never been reported before, these may be tested as potential anticancer drugs.

Keywords

G-quadruplex DNA; interactions; berberine and palmatine analogues; chemotherapy; NMR; FRET and MST assays

Subject

Chemistry and Materials Science, Medicinal Chemistry

Copyright: 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.

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