01861naa a2200337 a 450000100080000000500110000800800410001902400380006010000200009824500910011826000090020952009000021865000120111865000260113065000120115665000120116865000130118065300230119370000220121670000220123870000190126070000210127970000210130070000210132170000240134270000170136670000180138370000210140170000180142277300830144016838812018-05-15 2009 bl uuuu u00u1 u #d7 a10.1016/j.ejmech.2008.10.0252DOI1 aPINTO, A. C. S. aNew antimalarial and cytotoxic 4-nerolidylcatechol derivatives.h[electronic resource] c2009 a4-nerolidylcatechol (1) was isolated from cultivated Pothomorphe peltata root on a multi-gram scale using straight-forward solvent extraction-column chromatography. New semisynthetic 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,Odibenzoyl derivatives 2-8 exhibited IC50 in the 0.67?22.52 ìM 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. amalaria aPlasmodium falciparum aCaapeba aCâncer aQuímica aPlantas medicinais1 aSILVA, L. F. R. e1 aCAVALCANTI, B. C.1 aMELO, M. R. S.1 aCHAVES, F. C. M.1 aLOTUFO, L. V. C.1 aMORAIS, M. O. de1 aANDRADE-NETO, V. F.1 aTADEI, W. P.1 aPESSOA, C. O.1 aVIEIRA, P. P. R.1 aPOHLIT, A. M. tEuropean Journal of Medicinal Chemistrygv. 44, n. 6, p. 2731-2735, June 2009.