Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 44, Issue 6, Pages 2731-2735Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2008.10.025
Keywords
Plasmodium falciparum; Human colon carcinoma; Human nervous system cancer; Melanoma; Human myeloblastic leukemia; Semi-synthetic 4-nerolidylcatechol derivatives
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Funding
- FAPEAM [PIPT 006/2003, CBA-UFAM 1577/2005]
- POSGRAD
- PIBIC/INPA
- PPG-7/CNPq [557106/06]
- MCT/CNPq/PPBio [48.0002/04-5]
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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 I 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 mu M 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. (C) 2008 Elsevier Masson SAS. All rights reserved.
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