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Journal of Clinical & Experimental Pathology | ISSN: 2161-0681 | Volume 8
Breast Pathology and Cancer Diagnosis
6
th
World Congress and Expo on
July 25-26, 2018 | Vancouver, Canada
Medicinal Chemistry and Rational Drugs
20
th
International Conference on
&
Synthesis and biological evaluation of new a-ring modified asiatic acid derivatives as anticancer agents
Bruno M F Gonçalves
1, 2
, Samuel M Silvestre
2,3
, Sílvia Marín
4
, Marta Cascante
4
and
Jorge A R Salvador
1,5
1
CHEM4PHARMA, Portugal
2
Centre for Neuroscience and Cell Biology, Portugal
3
CICS-UBI – Health Sciences Research Centre, Portugal
4
Institute of Biomedicine, University of Barcelona, Spain
5
University of Coimbra, Portugal
C
ancer is one of the leading causes of mortality and morbidity worldwide. Despite major advances in diagnostics and therapeutics
of cancer, the the outcome for many patients remains limited. Thus, there is a constant demand for the search of new, safer
and effective pharmacological treatments to fight cancer. Asiatic acid (AA) is an pentacyclic triterpenoid that exhibited promising
anticancer effects in both
in vitro
and
in vivo
studies. In addition, this compound exhibited a relatively safe profile, and is readily
availability in nature, which support the contention that AA is an interesting compound for the design of new leads aimed at the
development of new anticancer agents. Hence, in the present work, a series of new lactol and A-nor AA derivatives were prepared, and
their antiproliferative activities were evaluated against several human cancer cell lines. Among all the derivatives tested, compound
1 exhibited the best antiproliferative profile, with IC50 values ranging from 0.11 µM to 0.65 µM for cancer cells. The results of the
preliminary mechanistic studies suggest that compound 1 induced cell cycle arrest at G0/G1 phase and apoptotic HeLa cell death. In
light of this results, compound 1 might represent a promising drug candidate for the development of new anticancer agents.
brunomfgoncalves@gmail.comJ Clin Exp Pathol 2018, Volume 8
DOI: 10.4172/2161-0681-C3-052