Use este identificador para citar ou linkar para este item: http://repositorio.inpa.gov.br/handle/123/3831
Título: New antimalarial and cytotoxic 4-nerolidylcatechol derivatives
Autor(es): Ana Cristina da Silva Pinto,
Pessoa, Claudia O.
Adrian Martin Pohlit
Silva, Luis Francisco Rocha
Bruno Coêlho Cavalcanti
Melo, Márcia Rúbia Silva
Francisco Célio Maia Chaves
Letícia Vera Costa Lotufo
Manoel Odorico de Moraes
Valter Ferreira de Andrade-Neto
Tadei, Wanderli Pedro
ISSN: 0223-5234
Revista: European Journal of Medicinal Chemistry
Volume: 44
Resumo: Nerolidylcatechol (1) was isolated from cultivated Pothomorphe peltata root on a multigram scale using straight-forward solvent extraction-column chromatography. New semi-synthetic derivatives of 1 were prepared and tested in vitro against multidrug-resistant Plasmodium falciparum K1 strain. Mono-O-methyl, mono-O-benzyl, O,O-dibenzyl and O,O-dibenzoyl derivatives 2–8 exhibited IC50 in the 0.67–22.52 μM range. Mono-O-methyl ethers 6 and 7 inhibited the in vitro growth of human tumor cell lines HCT-8 (colon carcinoma), SF-295 (central nervous system), LH-60 (human myeloblastic leukemia) and MDA/MB-435 (melanoma). In general, derivatives 2–8 are more stable to light, air and pH at ambient temperatures than their labile, natural precursor 1. These derivatives provide leads for the development of a novel class of antimalarial drugs with enhanced chemical and pharmacological properties.
URI: http://repositorio.inpa.gov.br/handle/123/3831
ISSN: 0223-5234
DOI: https://dx.doi.org/10.1016/j.ejmech.2008.10.025
Aparece nas coleções:Coordenação de Tecnologia e Inovação (COTI)

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