Synthesis and evaluation of PEGylated amino pyrimidines coated on gold and silver nanoparticles as drug delivery system for anticancer activity

Nitin K. Longadge and Anjali M

Abstract

A series of PEGylated amino pyrimidines surfaced on to gold and silver nanoparticles was designed, synthesized and evaluated for anticancer activity against three human cancer cell lines: U2OS osteosarcoma, MB231 breast cancer and SW480 colon carcinoma. Non-PEGylated and nanoparticles linked PEGylated pyrimidines exhibited moderate to potent activity against U2OS and MB231. Among them, the PEGylated amino pyrimidines showed excellent broad spectrum activity with IC50 values ranging from 13 to 346μM. Particularly, the PEGylated amino pyrimidines with thiophene ring at C2 showed significant potency against all tested human cancer cell lines. The morphology of all the compounds was tested by TEM and XRD. In this study, two independent approaches that conjugating pyrimidines to PEG(200) and mounting this passive targeting moieties onto the NPs were adopted to fabricate pyrimidine-PEG-AuNPs and pyrimidine-PEG-AgNPs. The NPs synthesized in this study were proven able to effectively target PEGylation to cancer cells, and showed profound apoptotic induction effect to those cells. Although the drug efficacy was compromised after conjugation with Au and Ag, the resultant could still make this moiety NPs a good candidate for anticancer therapy.