Ferrocene incorporated PAMAM dendrons: synthesis, characterization, and anti-cancer activity against AGS cell line
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Med Chem Res (2013) 22:4867–4876 DOI 10.1007/s00044-013-0491-x
ORIGINAL RESEARCH
Ferrocene incorporated PAMAM dendrons: synthesis, characterization, and anti-cancer activity against AGS cell line Tug˘ba Sag˘ır • Sevim Is¸ ık • Mehmet S¸ enel
Received: 4 October 2012 / Accepted: 11 January 2013 / Published online: 30 January 2013 Ó Springer Science+Business Media New York 2013
Abstract Novel series of asymmetric Poly(amidoamine) (PAMAM) dendrons containing a single ferrocene unit located as the focal point has been prepared. First, second, and third generation ferrocene-PAMAM dendrons with branched amine periphery and focal ferrocene functionality were synthesized via divergent pathways. The synthesized dendrons were characterized by FT-IR and NMR spectroscopy. Real-time cell analysis, cell viability, and anti-cancer activity of ferrocene-PAMAM dendrons were evaluated in AGS cells. While cell viability decreased, anti-cancer activity increased gradually in a dose-dependent manner in one, two, and three generations. Keywords Ferrocene PAMAM dendron Real-time cell analysis Anti-cancer activity
Introduction The therapeutic activity of drugs is often diminished by their poor solubility in the body’s aqueous compartment. To overcome this problem, the drug must be soluble in
Electronic supplementary material The online version of this article (doi:10.1007/s00044-013-0491-x) contains supplementary material, which is available to authorized users. T. Sag˘ır S. Is¸ ık (&) Department of Biology, Faculty of Arts and Sciences, Fatih University, B.Cekmece, Istanbul 34500, Turkey e-mail: [email protected] M. S¸ enel (&) Department of Chemistry, Faculty of Arts and Sciences, Fatih University, B.Cekmece, Istanbul 34500, Turkey e-mail: [email protected]
aqueous solutions which lead to its absorption at an optimum rate and facilitate the systemic delivery of the drug to the body. Different methods have been proposed to overcome the solubility problems of therapeutic agents (Hughey et al., 2011; Narayan, 2011; Buckley et al., 2012; Maddaford, 2012). Among the macromolecules, dendrons have been extensively used in drug delivery systems due to their highly branched, three dimensional, monodisperse structure, and controlled method of synthesis (Qiu and Bae, 2006; Zamboni, 2008; Gu, 2012; Wang and Grayson, 2012). Poly(amidoamine) (PAMAM), a type of dendron, have been widely studied in drug delivery because it allows the precise control of size, shape, placement of functional groups, minimum toxicity, and wide availability (Milhem et al., 2000; Muller and Schluter, 2005; Wu et al., 2011; Cortez-Maya et al., 2012; Zhang et al., 2012). Up to now, many solubility and drug delivery studies based on the PAMAM dendrons have been done such as sulfamethoxazole, doxorubicin, chlorambucil, 8-methoxypsoralene, and camptothecin (Ma et al., 2007; Cheng et al., 2008; Borowska et al., 2010; Bielawski et al., 2011; Chang et al., 2011). Since its accidental discovery in 1951, many ferrocene derivatives have been synthesized and charac
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