alexa
Reach Us +1-947-333-4405
Design, Synthesis And Biological Evaluation Of Novel Celastrol Derivatives As Potent And Selective Cytotoxic Compounds | 92092
ISSN: 2161-0681

Journal of Clinical & Experimental Pathology
Open Access

Like us on:

OMICS International organises 3000+ Global Conferenceseries Events every year across USA, Europe & Asia with support from 1000 more scientific Societies and Publishes 700+ Open Access Journals which contains over 50000 eminent personalities, reputed scientists as editorial board members.

Open Access Journals gaining more Readers and Citations
700 Journals and 15,000,000 Readers Each Journal is getting 25,000+ Readers

This Readership is 10 times more when compared to other Subscription Journals (Source: Google Analytics)
All submissions of the EM system will be redirected to Online Manuscript Submission System. Authors are requested to submit articles directly to Online Manuscript Submission System of respective journal.

Design, synthesis and biological evaluation of novel celastrol derivatives as potent and selective cytotoxic compounds

Joint Event on 6th World Congress and Expo on Breast Pathology and Cancer Diagnosis & 20th International Conference on Medicinal Chemistry and Rational Drugs

Jorge A R Salvador, Sandra AC Figueiredo, Vanessa, S Mendes, Roldan Cortes, Marta Cascante and Jorge A R Salvador

University of Coimbra, Portugal Centre for Neuroscience and Cell Biology, Portugal Biocant - Parque Tecnologico de Cantanhede, Portugal University of Barcelona, Spain

Posters & Accepted Abstracts: J Clin Exp Pathol

DOI: 10.4172/2161-0681-C3-052

Abstract
Triterpenoids comprise a large and structurally diverse class of natural products. Among these, celastrol is one of the most active antitumour compounds. It has been reported to be highly active against a wide variety of tumours and to affect multiple cellular pathways. Therefore, celastrol is an ideal candidate for designing lead compounds for the development of new anticancer agents. In this communication we report the synthesis of novel celastrol derivatives as potent and selective cytotoxic compounds. Celastrol analogues, including carbamate derivatives, were designed and synthesised, and their anticancer activity was evaluated using different human cancer cell lines. Moreover, these new compounds were subjected to a preliminary structure–activity relationship study. The best derivatives were selected considering their best activity on malignant cell viability, combined with the highest selectivity between cancer cells and non-malignant fibroblasts. It was performed preliminary mechanistic studies with the best compound, which indicated a important cytotoxic effect on SKOV-3 human ovarian cancer cells (IC50 = 0.54 μM). Additionally, the results suggested that this compound presented an antiapoptotic activity, mediated mainly through activation of extrinsic apoptotic pathway. Furthermore, our results demonstrated the potential of this derivative as a new agent for combinatorial drug therapy for ovarian cancer.
Biography

Jorge A R Salvador has a degree in Pharmaceutical Sciences, a Master degree in Organic & Tecnological Chemistry, and a Ph.D. in Pharmaceutical Chemistry from the University of Coimbra in collaboration with the University of York, UK. He has a position as Full Professor at Faculty of Pharmacy of the University of Coimbra – Portugal. Author and co-author of over 90 publications in peer-review journals, 10 book chapters and 10 patents, two of them have been granted in US. Co-founder of the company CHEM4PHARMA, Lda, https://www.chem4pharma.com/.

E-mail: [email protected]

Top