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https://repositorio.inpa.gov.br/handle/1/18433| Título: | New antimalarial and cytotoxic 4-nerolidylcatechol derivatives |
| Autor: | Pinto, Ana Cristina da Silva Silva, Luis Francisco Rocha Coelho Cavalcanti, Bruno Melo, Márcia R.S. Chaves, Francisco Célio Maia Costa-Lotufo, Leticia Veras Moraes, Manœl Odorico de Andrade Neto, Valter Ferreira de Tadei, Wanderli Pedro Pessoa, Cláudia do Ó. Vieira, Pedro Paulo Ribeiro Pohlit, Adrian Martin |
| Palavras-chave: | 1 O Methyl 4 Nerolidylcatechol 2 O Methyl 4 Nerolidylcatechol 4 Nerolidylcatechol Antimalarial Agent Doxorubicin O,o Dibenzoyl 4 Nerolidylcatechol O,o Dibenzyl 4 Nerolidylcatechol Unclassified Drug Column Chromatography Controlled Study Cytotoxicity Drug Isolation Drug Stability Environmental Temperature Human Human Cell Ic 50 Malaria Medicinal Plant Ph Measurement Plasmodium Falciparum Pothomorphe Peltata Solvent Extraction Animal Antimalarials Antineoplastic Agents, Phytogenic Catechols Cell Line, Tumor Cell Proliferation Dose-response Relationship, Drug Drug Resistance Drug Screening Assays, Antitumor Hl-60 Cells Humans Molecular Structure Parasitic Sensitivity Tests Piperaceae Plant Extracts Plant Roots Plasmodium Falciparum Stereoisomerism |
| Data do documento: | 2009 |
| Revista: | European Journal of Medicinal Chemistry |
| É parte de: | Volume 44, Número 6, Pags. 2731-2735 |
| Abstract: | 4-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. © 2008 Elsevier Masson SAS. All rights reserved. |
| DOI: | 10.1016/j.ejmech.2008.10.025 |
| Aparece nas coleções: | Artigos |
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