Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 79, Issue -, Pages 110-116Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.03.086
Keywords
R-(+)-limonene; Thiosemicarbazide; Thiosemicarbazones; Antitumor; Prostate cancer cells
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Funding
- Fundacao Araucaria (Parana-Brazil) [15787/2008]
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq, Brazil) [477069-2008-8]
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In an attempt to develop potent and selective antitumor agents, a series of novel thiosemicarbazones derived from a natural monoterpene R-(+)-limonene was synthesized and their antitumor activity was evaluated. Overall, the majority of tested compounds exhibited considerable inhibitory effects on the growth of a wide range of cancer cell lines. Almost all of tested thiosemicarbazones were especially sensitive to prostate cells (PC-3). Derivatives 5, 6, 8, 9, 10, 11 and 13 presented the most potent antitumor activity against PC-3 cells. These compounds showed lower value of GI(50) (0.04-0.05 mu M) than the reference drug paclitaxel, besides a high selectivity for the same cell line. The 4-fluorobenzaldehyde derivative 10 was the most selective compound for prostate cells, while 2-hydroxybenzaldehyde derivative 8 was the most active compound, with potent antitumor activity against all tested cell lines. (C) 2014 Elsevier Masson SAS. All rights reserved.
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