Ability of Group IVB metallocene polyethers containing dienestrol to arrest the growth of selected cancer cell lines

<p>Abstract</p> <p>Background</p> <p>Monomeric Group IVB (Ti, Zr and Hf) metallocenes represent a new class of antitumor compounds. There is literature on the general biological activities of some organotin compounds. Unfortunately, there is little information with respect to the molecular level activity of these organotin compounds. We recently started focusing on the anti-cancer activity of organotin polymers that we had made for other purposes and as part of our platinum anti-cancer effort.</p> <p>Methods</p> <p>For this study, we synthesized a new series of metallocene-containing compounds coupling the metallocene unit with dienestrol, a synthetic, nonsteroidal estrogen. This is part of our effort to couple known moieties that offer antitumor activity with biologically active units hoping to increase the biological activity of the combination. The materials were confirmed to be polymeric using light scattering photometry and the structural repeat unit was verified employing matrix assisted laser desorption ionization mass spectrometry and infrared spectroscopy results.</p> <p>Results</p> <p>The polymers demonstrated the ability to suppress the growth of a series of tumor cell lines originating from breast, colon, prostrate, and lung cancers at concentrations generally lower than those required for inhibition of cell growth by the commonly used antitumor drug cisplatin.</p> <p>Conclusion</p> <p>These drugs show great promise in vitro against a number of cancer cell lines and due to their polymeric nature will most likely be less toxic than currently used metal-containing drugs such as cisplatin. These drugs also offer several addition positive aspects. First, the reactants are commercially available so that additional synthetic steps are not needed. Second, synthesis of the polymer is rapid, occurring within about 15 seconds. Third, the interfacial synthetic system is already industrially employed in the synthesis of aromatic nylons and polycarbonates. Thus, the ability to synthesize large amounts of the drugs is straight forward.</p

Mössbauer Spectroscopy and Organotin Polymers

Mössbauer spectroscopy allows the structural analysis of certain metal atoms situated in complex structures. Briefly, Mössbauer spectroscopy is a resonant absorption spectroscopy that is observed best in isotopes having long lived, low-lying excited nuclear energy states. The largest recoil-free resonant cross-section is found for 57Fe. Currently, Mössbauer spectroscopy is being used on Mars to identify iron compounds that are present in the Martian landscape. There are over 20,000 entries in SciFinder for Mössbauer spectroscopy, of which the two largest entries are for iron and tin containing compounds. There are only about 100 entries for organotin compounds, with only a handful related to organotin-containing polymers. Mössbauer spectroscopy is an extremely powerful structural characterization tool that has been greatly overlooked because each Mössbauer spectrometer must be dedicated to a single element and measurements generally take hours to days to complete. This chapter deals with the study of a particular potentially important set of organotin polymers that illustrates the strength of this spectral technique

Ciprofloxacin Polymers Derived from Diallyltin and Divinyltin Dihalides

The initial synthesis of condensation polymers from newly available divinyltin dichloride and diallyltin dichloride and ciprofloxacin is accomplished employing a modified interfacial polycondensation process. The polymeric (DP are about 2,000) products are rapidly (less than 15 seconds) formed in good yield. Infrared spectroscopy shows the formation of Sn-O and Sn-N bonds as predicted from the proposed structure. F-MALDI MS also shows ion fragments containing organotin in the predicted isotopic abundances as well as ion fragments containing both organotin and ciprofloxacin. The polymers exhibit low toxicity towards healthy WI-38 cells with variable toxicities towards a variety of cancer cell lines