Please use this identifier to cite or link to this item: https://repositorio.inpa.gov.br/handle/1/18433
Title: New antimalarial and cytotoxic 4-nerolidylcatechol derivatives
Authors: 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
Keywords: 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
Issue Date: 2009
metadata.dc.publisher.journal: European Journal of Medicinal Chemistry
metadata.dc.relation.ispartof: 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.
metadata.dc.identifier.doi: 10.1016/j.ejmech.2008.10.025
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