Abstract
An architectural polymer containing hydrophobic isoxazole-based dendron and hydrophilic polyethylene glycol linear tail is prepared by a combination of the robust ZnCl2 catalyzed alkyne-nitrile oxide 1,3-dipolar cycloaddition and esterification chemistry. This water soluble amphiphilic telodendrimer acts as a macromolecular biologically active agent and shows concentration dependent reduction of glioblastoma (U251) cell survival.
Highlights
The isoxazole moiety, a five-membered heterocycle containing oxygen and nitrogen at adjacent positions, has shown interesting biological properties including anticancer [1], antimicrobial [1], antibacterial [2], anti-inflammatory [3], antiviral [4], antithrombic [5], antiapoptotic [6] and antiparasitic activity [7]
We first explored the potential of 1,3-dipolar cycloaddition strategy in the synthesis of a symmetric generation 0 dendrimer
We first explored the potential of 1,3-dipolar cycloaddition strategy in the synthesis of a with potassium hydroxide in dry DMF (Scheme 1) [32], followed by the 1,3-dipolar cycloaddition symmetric generation 0 dendrimer
Summary
The isoxazole moiety, a five-membered heterocycle containing oxygen and nitrogen at adjacent positions, has shown interesting biological properties including anticancer [1], antimicrobial [1], antibacterial [2], anti-inflammatory [3], antiviral [4], antithrombic [5], antiapoptotic [6] and antiparasitic activity [7]. NVP-AUY922 (Figure 1A) is an anticancer agent [1] and thiophen-2-yl isoxazole (Figure 1B) significantly inhibits proliferation of HeLa cells. Isoxazole with a steroid moiety (Figure 1C) has displayed considerable cytotoxicity towards tumor cell lines and sulfisoxazole, flucloxacillin, dicloxacillin, oxacillin, sulfamethoxazole and cloxacillin are some examples of marketed antimicrobial drugs bearing an isoxazole ring [8]. Macromolecular therapeutics are increasingly proposed as nanomedicines [19] and new methodologies to prepare highly potent isoxazoles bearing nanocarriers and nanotherapeutics will likely expand the scope of their applications
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