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May 13-14, 2019 | Prague, Czech Republic
Chemistry and Medicinal Chemistry
9th World Congress on
Asian Journal of Biomedical and Pharmaceutical Sciences | Volume 9 ISSN: 2249-622X
20 years of G-quadruplex ligands: From synthesis to relevant biological activity
Marco Franceschin
University of Rome, Italy
G -Quadruplexes represent a group of unusual DNA
secondary structures, based on Hoogsteen G–G paired
hydrophobic planar rings consisting of four guanine units.
Many studies have shown that G-quadruplex structures
appear to be involved in several important biological
processes, such as DNA replication, gene expression and
recombination, as well as cell transformation. Some of the
firstG-quadruplexligands(namelyperyleneandanthracene
derivatives) were published by L.H. Hurleyand S. Neidle in
1998/1999. Starting from 2001, inspired by their works, we
synthesized several perylene derivatives with different side
chains and studied their chemical properties and biological
activity, with the aim to understand the relevant molecular
features. In the following years, based on these results and
through improved syntheses, we prepared novel and more
promising aromatic compounds: berberine and palmatine
derivatives (from natural compounds), triazatruxene,
xanthene and xanthone derived compounds, as well
as, more recently, coronene derivatives. After 20 years,
some of these compounds have shown very interesting
biological effects, based on their ability to bind specific
G-quadruplex structures, both on telomers, affecting
therefore telomerase activity, and on oncogene promoting
sequences, leading to antiproliferative effects and thus
representing new potential selective anticancer drugs. In
this Keynote Speech, an overview of the most interesting
results will be given in order to understand future
perspectives.
Speaker Biography
Marco Franceschin graduated cum laude from the 'Sapienza' in 2001,
where he successively earned a PhD degree in Chemistry in 2005,
including a significant period of research activity at the School of
Pharmacy, University College London. Until 2011 he was a post-doc in
the same University of Rome: with over 10 years research experience in
the field of G-quadruplex ligands, leading to more than 30 international
publications (h-index 18). His work included organic synthesis,
characterization of the synthesized compounds and the study of DNA/
ligand interactions by means of gel electrophoresis, spectroscopic
techniques, molecular modeling simulations and mass spectrometry,
as well as their biological activity. He has been qualified as associate
professor of both Organic Chemistry and Medicinal Chemistry, holding
a temporary teaching position as professor of organic chemistry for
students in Biotechnology at the Faculty of Sciences of the University of
Rome 'Sapienza' from 2014 to 2018.
e:
Marco Franceschin, Asian J Biomed Pharmaceut Sci, Volume:9
DOI: 10.4066/2249-622X-C2-020
Notes: