Ferrocene-indole hybrids for cancer and malaria therapy |
| |
| Authors: | Josefina Quirante Faustine Dubar Asensio González Marta Cascante Isabelle Forfar Christophe Biot |
| |
| Institution: | a Laboratori de Química Orgànica, Facultat de Farmàcia, Institut de Biomedicina, (IBUB), Universitat de Barcelona, Barcelona, Spainb Université de Lille1, Unité de Catalyse et Chimie du Solide-UMR CNRS 8181, ENSCL, Bâtiment C7, B.P. 90108, 59652 Villeneuve d’Ascq Cedex, Francec Departament de Química Inorgànica, Facultat de Química, Universitat de Barcelona, Martí i Franquès 1-11. E-08028-Barcelona, Spaind Department of Biochemistry and Molecular Biology, Faculty of Biology, Institute of Biomedicine of University of Barcelona (IBUB) and IDIBAPS, Unit Associated with CSIC, Diagonal 645, 08028 Barcelona, Spaine Université de Bordeaux, Pharmacochimie EA 4138, Bordeaux, Francef Institut de Recherche Biomédicale des Armées, Antenne de Marseille, Unité de Recherche en Biologie et Epidémiologie Parasitaires, URMITE-UMR 6236, Allée du Médecin Colonel Jamot, Parc le Pharo, BP 60109, 13262 Marseille Cedex 07, France |
| |
| Abstract: | We report the synthesis, characterization, and cytotoxic and antimalarial activity of ferrocene-indole hybrids 8-14. The 2-phenylindole scaffold was chosen because of its potent antimitotic activity and ferrocene was chosen following the development of ferrocifens, ferrocene derivatives of tamoxifen, which are prototypes of a new family of organometallic anti-estrogens. Ferrocene-indole hybrids 8-14 and their corresponding organic analogues 1-7 showed only moderate antimalarial activities, while ferrocene-indole hybrids 11 and 12 showed excellent in vitro activities against the A549 human carcinoma cell line, with IC50 values of 5 and 7 μM respectively. These ferrocene-indole hybrids were up to 25-fold more potent as cytotoxic agents than their purely organic analogues. |
| |
| Keywords: | Cancer Malaria Hybrid drug Indole Ferrocene |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
