www.victoria.ac.nz/ferrier www.victoria.ac.nz/ferrier www.glycosyn.com http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 http://dx.doi.org/doi:10.1002/cmdc.201600270 15/2016 www.chemmedchem.org A J ournal of Cover Picture: P. M. Rendle et al. Poly Ethoxy Ethyl Glycinamide (PEE-G) Dendrimers: cally Designed for Pharmaceutical Applications Dendrimers are large, banched molecules with well-defined structure. They can be can be conjugated to or used to encapsulate therapeutic drugs or imaging moieties or may also be used as drugs in their own right. PEE-G dendrimers have been designed to be: Stable No observable degradation of G4 PEE-G CO 2 H after 24 hrs at 40 °C, neat or in PBS. Non-toxic Observed to have low cytotoxicity, low immunogenicity and acute tolerated dose in adult rats of >1000 mg/kg Pure High purity by HPLC and being constantly improved Scalable Made from cheap, readily available starting materials via an efficient, scalable, convergent synthesis Water soluble G4 PEE-G CO 2 H soluble in PBS at >400 mg/mL Flexible Long linkers between branching points giving a ‘low density’, long reach dendrimer Variations Free acid centre and/or free amine terminals. Carboxylic acid (mono or di) capped terminals. Alternating amine and hydroxy terminals. Our partners, GlycoSyn, have the ability to manufacture on kilogram scale and under GMP to provide products suitable for human clinical trials. PEE-G dendrimers can be purchased online: www.glycofinechem.glycosyn.com/collections/dendrimers The scaffold is patent protected and available for licensing. Contact Stephen Lorimer: [email protected]. Macromolecular scaffolds specifically designed for pharmaceutical applicatons PEE-G dendrimers O NHBoc O NHBoc O NHBoc O NHBoc O H N O N O N H O N NH O N O NH O O O BnO O NHBoc O NHBoc O NHBoc O NHBoc O H N O N O N H O N N O HN O N N O HN O O NHBoc O NHBoc O NHBoc O NHBoc O H N O N O N H O N O NHBoc O NHBoc O NHBoc O NHBoc O H N O N O N H O N N O HN O N N O HN O G4 BnO PEE-G NHBoc 4 6 8 10 12 14 16 18 20 0 10 20 30 40 50 98.6% 96.7% 94.4% 91.1% G1 HO PEE-G NHBoc G2 HO PEE-G NHBoc G3 HO PEE-G NHBoc Time / min G4 HO PEE-G NHBoc HPLC-CAD April 2017