Our group has a long researching tradition in the field of organotin(IV) complexes, usually proposed and tested as potential anti-tumor drugs. The leitmotif has usually been the modulation of the intrinsic toxicity/cytotoxicity of the organometallic moiety and a modulation of the toxic effect by means of biologically related molecules (synthetic or natural). Such a modulation is usually achieved by two (often overlapping) routes: dampen the damaging effects of the metal core, and serving as a carrier for specific tissue districts. Since a too tight binding on the organotin moiety is not always desirable – a too much stable complex could be a non-active one – carboxylates have always played an important role in our research, as attested by many papers. In the past, the carboxylic function has been used as an anchor for the tin, leaving to other functional groups the “biological” tasks; in this work, though, is directed towards some simple – aliphatic chain, no other functional (coordinating) groups – carboxylic acids, such as butyric or valproic acid. Even in their simplicity, those acids were chosen because of their anion activity as histone deacetylase inhibitors, and, as such, are used as adjunct in cancer treatment. Similarly to other previously studied simple acids (unpublished results), a large difference occurs in di- and tri-organo compounds, but in a constant pattern. This presentation deals with some preliminary structural characterization and biological assays.
Scopelliti, M., Fiore, T., Pellerito, C., Casella, G., Prinzivalli, C., Giuliano, M., et al. (2012). Organotin(IV) and simple fatty acids: preliminary assessments. In 12th Workshop on Pharmacobiometallics (pp.47-47). Padova.
Organotin(IV) and simple fatty acids: preliminary assessments
SCOPELLITI, Michelangelo;FIORE, Tiziana;PELLERITO, Claudia;CASELLA, Girolamo;PRINZIVALLI, Cristina;GIULIANO, Michela;CALVARUSO, Giuseppe;PELLERITO, Lorenzo
2012-01-01
Abstract
Our group has a long researching tradition in the field of organotin(IV) complexes, usually proposed and tested as potential anti-tumor drugs. The leitmotif has usually been the modulation of the intrinsic toxicity/cytotoxicity of the organometallic moiety and a modulation of the toxic effect by means of biologically related molecules (synthetic or natural). Such a modulation is usually achieved by two (often overlapping) routes: dampen the damaging effects of the metal core, and serving as a carrier for specific tissue districts. Since a too tight binding on the organotin moiety is not always desirable – a too much stable complex could be a non-active one – carboxylates have always played an important role in our research, as attested by many papers. In the past, the carboxylic function has been used as an anchor for the tin, leaving to other functional groups the “biological” tasks; in this work, though, is directed towards some simple – aliphatic chain, no other functional (coordinating) groups – carboxylic acids, such as butyric or valproic acid. Even in their simplicity, those acids were chosen because of their anion activity as histone deacetylase inhibitors, and, as such, are used as adjunct in cancer treatment. Similarly to other previously studied simple acids (unpublished results), a large difference occurs in di- and tri-organo compounds, but in a constant pattern. This presentation deals with some preliminary structural characterization and biological assays.File | Dimensione | Formato | |
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