Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 23, Issue 13, Pages 3687-3695Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2015.04.015
Keywords
Synthesis; Ent-kaurane; Caracasine acid; Cytotoxic activity; Antileishmanial; Antitrypanosomal; Antibacterial
Funding
- FONACIT [PEII-705, P-2013000385]
- Venezuelan Ministry of Higher Education, Science, and Technology (IDEA Foundation) [POA-2013]
- National Fund for Endogenous Development (Fonden-Venezuela)
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A series of caracasine acid (1) derivatives were synthesized and evaluated for their in vitro cytotoxicity on human cancer-derived cell lines MCF-7 and PC-3, as well as for other activities such as antibacterial, antileishmanial and antitrypanosomal activity. Compound 1 was more effective than any of its derivatives against tested human cancer cell lines. PC-3 cells were more sensitive than MCF-7 to all compounds, particularly the methyl ester (2), the amide (9) and the epoxide (10). The evaluation of antiparasitic activity revealed that ester derivatives (2-8) and the amide derivative (9) were the most effective antileishmanial and antitrypanosomal compounds, even though their effect on Trypanosoma cruzi was modest. Finally, compound 1 and the derivatives evidenced a broad spectrum of antibacterial activity, as assayed against Gram-positive and Gram-negative bacteria. (C) 2015 Elsevier Ltd. All rights reserved.
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