Synthesis and biological evaluation of caracasine acid derivatives.
Basic Information
ID: ALA3585240
Journal: Bioorg Med Chem
Title: Synthesis and biological evaluation of caracasine acid derivatives.
Authors: Chávez K, Compagnone RS, Álvarez A, Figarella K, Galindo-Castro I, Marsiccobetre S, Triviño J, Arocha I, Taddei A, Orsini G, Tillett S, Suárez AI.
Abstract: 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.
CiteXplore: 25891984
DOI: 10.1016/j.bmc.2015.04.015
Patent ID: ┄