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Eur J Med Chem ; 44(6): 2731-5, 2009 Jun.
Article in English | MEDLINE | ID: mdl-19084293

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 IC(50) in the 0.67-22.52 microM 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.


Subject(s)
Antimalarials/pharmacology , Antineoplastic Agents, Phytogenic/pharmacology , Catechols/pharmacology , Plant Extracts/pharmacology , Plasmodium falciparum/drug effects , Animals , Antimalarials/chemical synthesis , Antimalarials/chemistry , Antimalarials/toxicity , Antineoplastic Agents, Phytogenic/chemical synthesis , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/toxicity , Catechols/chemical synthesis , Catechols/chemistry , Catechols/toxicity , Cell Line, Tumor , Cell Proliferation/drug effects , Dose-Response Relationship, Drug , Drug Resistance , Drug Screening Assays, Antitumor , HL-60 Cells , Humans , Molecular Structure , Parasitic Sensitivity Tests , Piperaceae/chemistry , Plant Extracts/chemical synthesis , Plant Extracts/chemistry , Plant Extracts/toxicity , Plant Roots/chemistry , Stereoisomerism
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