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Medchem & Toxicology 2018
Page 26
Journal of Organic & Inorganic Chemistry
ISSN: 2472-1123
A n n u a l C o n g r e s s o n
Medicinal Chemistry,
Pharmacology and toxicology
J u l y 3 0 - 3 1 , 2 0 1 8
Am s t e r d a m , N e t h e r l a n d s
H
uman papillomavirus (HPV) infection is now a well-established cause of
different types of cancer including but not limited to cervical cancer. There
are currently no specific treatments for patients with HPV-driven cancers. One
common denominator of the HPV genotypes is the E6 and E7 proteins, which
are mainly responsible for malignant and non-malignant phenotypes. Hence,
they represent valuable targets for therapeutic intervention in HPV-driven
cancers. We have already successfully shown a natural diterpenoid, anisomelic
acid (AA) down-regulates E6 and E7 oncoproteins, leading to efficient inhibition
of cell growth and induction of apoptosis. During the optimization of AA
synthesis, we have identified few small molecules, which preferentially targets
the HPV E6 and E7 proteins similar to AA mode of action, but, more efficient
than AA in inducing apoptosis in cervical cancer cells. Furthermore, these 'HIT'
molecules also showed specificity in killing HPV positive cells with different
genotypes compared with human primary skin fibroblast cells. Indeed, cancer
xenograft models in nude mice demonstrated proof of principle, where a
decrease in tumour size was observed in HPV-driven tumours treated with our
HIT compound(s).
Biography
YuryBrusentsevobtainedhisMaster’sdegree inChemistryfrom
Moscow State University in 2003. He worked as a Researcher in
R&D (drug development) for Pharmaceutical industry until 2009
and moved back to academia and received his PhD in 2017,
the group of Patrik Eklund at Abo Akademi University. Now he
is carrying out chemistry part of the drug discovery projects
(drug design and synthesis of drug candidates) as a Postdoc
researcher. His research interests are in Medicinal Chemistry,
Advanced Organic Synthesis and Organometallic Chemistry.
ybrusent@abo.fiSynthesis and evaluation of anisomelic acid like compounds for
the treatment of HPV-mediated carcinomas
Rajendran Senthilkumar
1
, Yury Brusentsev
2
, Preethy Paul
1
, Fang
Cheng
1
, Maria Sippola-Thiele
1
, Patrik Eklund
2
and John E Eriksson
1
1
Turku Centre of Biotechnology, Finland
2
Abo Akademi University, Finland
Yury Brusentsev et al., J Org Inorg Chem 2018, Volume 4
DOI: 10.21767/2472-1123-C3-008