Synthesis and antiproliferative activity of novel limonene derivatives with a substituted thiourea moiety

A series of R-(+)-limonene derivatives bearing a substituted thiourea moiety (3-13) and five S-methyl analogs (14-18) were synthesized and evaluated for their in vitro antiproliferative activity against human cancer cell lines. Compounds bearing aromatic substituents (3-6) exhibit cytotastic activity in the full panel of cell lines tested, with GI50 values in the range of 2.5 to 24 µmol L-1. Compounds 3, 10, 12 and 16 were the most active with GI50 values in the range of 0.41 to 3.0 µmol L-1, against different cell lines.No presente trabalho descrevemos a síntese e a avaliação da atividade antiproliferativa, frente a linhagens de células tumorais humanas, de derivados do R-(+)-limoneno (3-18) contendo uma unidade tiouréia substituída. Os derivados com substituintes arílicos (3-6) exibiram atividade citostática frente a todas linhagens testadas, com inibição de 50% do crescimento celular (GI50) em concentrações na faixa de 2,5 a 24 µmol L-1. Os compostos 3, 10, 12 e 16 foram os mais ativos, com GI50 na faixa de 0,41 a 3,0 mmol L-1, frente a diferentes linhagens celulares.954960Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES

Qualitative determination of indole alkaloids of Tabernaemontana fuchsiaefolia (Apocynaceae)

This paper describes a fast and efficient procedure to separate and identify indole alkaloids from the ethanolic extract of Tabernaemontana fuchsiaefolia (Apocynaceae). The alkaloidal fractions obtained from ethanolic extracts of leaves and stem barks and root barks were fractioned and analyzed by Thin-Layer Chromatography (TLC) and by Gas Chromatography coupled to Mass Spectrometry (GC-MS). The following indole alkaloids were identified: ibogamine, coronaridine, ibogaine pseudoindoxyl, voacangine hydroxyindolenine, voacangine pseudoindoxyl, tabernanthine, catharanthine, voacangine, 19-oxovoacangine, 10-hydroxycoronaridine, affinisine, 16-epi-affinine, voachalotine, ibogaline, and conopharyngine

Synthesis and antitumor activity of novel 1-substituted 3-(4,5-substituted 1,2,4-triazol-3-yl)--carboline derivatives

Schiff bases, 1,2,4-triazolo[4,3- d ][1,2,3,4]thiatriazoles, and 1,2,4-triazolo[3,4- b ][1,3,4]thiadiazoles carrying the -carboline nucleus were synthesized from 3-(4-amino-5-mercapto-1,2,4-triazol-3-yl)--carbolines. The compounds were evaluated for their in vitro antitumor activity against eight human cancer cell lines. The 1,2,4-triazolo[4,3- d ][1,2,3,4]thiatriazole derivatives showed a broad spectrum of antitumor activity, with GI (50) values lower than 13 M for all cell lines tested. In general, all tested compounds showed potent activity against the breast (MCF-7) cancer cell line, with GI (50) values in the range of 2.07 to 4.58M512573577FAPESP – Fundação de Amparo à Pesquisa Do Estado De São PauloSem informaçã