Utilize este identificador para referenciar este registo: http://hdl.handle.net/10451/21632
Título: Cryptolepine analogues containing basic aminoalkyl side-chains at C-11
Synthesis, antiplasmodial activity, and cytotoxicity
Autor: Lavrado, Joao
Paulo, Alexandra
Gut, Jiri
Rosenthal, Philip J.
Moreira, Rui
Palavras-chave: Chemistry, Medicinal
Chemistry, Organic
Data: 2008
Editora: PERGAMON-ELSEVIER SCIENCE LTD
Citação: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - Vol. 18, n. 4 (FEB 15 2008), p. 1378-1381
Resumo: A series of cryptolepine derivatives has been synthesized through the incorporation of short basic side-chains in the C-11 position of the 10H-indolo[3,2-b] quinoline scaffold. Their antiplasmodial activity was evaluated in vitro against the chloroquine resistant Plasmodium falciparum W2 strain, showing IC50 values between 22 and 184 nM, while their cytotoxicity was assessed using HUVEC cells, revealing three compounds with a selectivity ratio higher than 10. The most selective of these derivatives, 4d, with a selectivity ratio of 46, was also the least cytotoxic of the series. (c) 2008 Elsevier Ltd. All rights reserved.
URI: http://hdl.handle.net/10451/21632
DOI: http://dx.doi.org/10.1016/j.bmcl.2008.01.015
ISSN: 0960-894X
Aparece nas colecções:FF - Produção Científica 2000-2009

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