Utilize este identificador para referenciar este registo: http://hdl.handle.net/10451/17910
Título: Enhancing Macrocyclic Diterpenes as Multidrug-Resistance Reversers: Structure–Activity Studies on Jolkinol D Derivatives
Autor: Reis, Mariana
Ferreira, Ricardo J.
Santos, Maria M. M.
Molnár, J.
Santos, Daniel J. V. A.
Ferreira, M. J. U.
Data: 2013
Citação: Journal of Medicinal Chemistry. 2013, 56(3):748−760
Resumo: The phytochemical study of Euphorbia piscatoria yielded jolkinol D (1) in a large amount, whose derivatization gave rise to 12 ester derivatives (2–13) and hydrolysis to compound 14. The in vitro modulation of P-gp of compounds 1–14 was evaluated through a combination of transport and chemosensitivity assays, using the L5178 mouse T lymphoma cell line transfected with the human MDR1 gene. Apart from jolkinol D, all derivatives (2–14) showed potential as MDR reversal agents. In this small library of novel bioactive macrocyclic lathyrane diterpene derivatives, designed to evaluate structure–activity relationships essential in overcoming multidrug resistance (MDR), some correlations between MDR reversal and molecular weight, accessible solvent areas, and octanol/water partition coefficient were identified that can contribute to the development of new selective P-gp reversal agents.
Peer review: yes
URI: http://hdl.handle.net/10451/17910
DOI: http://dx.doi.org/10.1021/jm301441w
ISSN: 0022-2623
1520-4804
Versão do Editor: http://pubs.acs.org/doi/abs/10.1021/jm301441w
Aparece nas colecções:FF - Artigos em Revistas Internacionais

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