5842-08-0Relevant academic research and scientific papers
LIPOCATIONIC POLYMERS AND USES THEREOF
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Page/Page column 46;47, (2016/07/05)
Polymers produced by ring opening polymerization which comprises an amino group that can be used in compositions to deliver a nucleic acid such as a miRNA or a siRNA. In some embodiments, compositions which comprise the polymers described herein and a nucleic acid are also provided herein. In some embodiments, these compositions are used to silence one or more genes in vivo or treat a disease or disorder.
Rapid Synthesis of a Lipocationic Polyester Library via Ring-Opening Polymerization of Functional Valerolactones for Efficacious siRNA Delivery
Hao, Jing,Kos, Petra,Zhou, Kejin,Miller, Jason B.,Xue, Lian,Yan, Yunfeng,Xiong, Hu,Elkassih, Sussana,Siegwart, Daniel J.
supporting information, p. 9206 - 9209 (2015/08/06)
The ability to control chemical functionality is an exciting feature of modern polymer science that enables precise design of drug delivery systems. Ring-opening polymerization of functional monomers has emerged as a versatile method to prepare clinically translatable degradable polyesters.1 A variety of functional groups have been introduced into lactones; however, the direct polymerization of tertiary amine functionalized cyclic esters has remained elusive. We report a strategy that enabled the rapid synthesis of >130 lipocationic polyesters directly from functional monomers without protecting groups. These polymers are highly effective for siRNA delivery at low doses in vitro and in vivo.
'3+1' Mixed-ligand oxotechnetium(V) complexes with affinity for melanoma: Synthesis and evaluation in vitro and in vivo
Friebe, Matthias,Mahmood, Ashfaq,Spies, Hartmut,Berger, Ralf,Johannsen, Bernd,Mohammed, Ashour,Eisenhut, Michael,Bolzati, Cristina,Davison, Alan,Jones, Alun G.
, p. 2745 - 2752 (2007/10/03)
'3+1' Mixed-ligand [99mTc]oxotechnetium complexes with affinity for melanoma were synthesized in a one-pot reaction. Complexation of technetium-99m with a mixture of N-R(3- azapentane-1,5-dithiol) [R = Me, Pr, Bn, Et2N(CH2)2] and N-(2- dialkylamino)ethanethiol [alkyl = X = Et, Bu, morpholinyl] using Sn2+ as the reducing agent resulted in the formation of '3+1' mixed-ligand technetium-99m complexes [TcO(SN(R)S)(SNX2)] in high radiochemical yield (60-98%). In vitro uptake studies in B16 murine melanoma cells indicated a moderate tumor-cell accumulation (40%) of compound 1 [R = Me, X = Et] and a higher accumulation (69%) of compound 2 [R = Me, X = Bu] after a 60-min incubation. In vivo evaluation of compounds 1-6 in the C57B16/B16 mouse melanoma model demonstrated tumor localization. Compound 2 displayed the highest accumulation with up to 5% ID/g at 60 min after injection. In vivo, 2 also showed a low blood-pool activity and high melanoma/spleen (4.3) and melanoma/lung (1.9) ratios at 1 h. These results suggest that small technetium-99m complexes could be useful as potential melanoma-imaging agents.
