Abstract:
Phenothiazine based compounds are well known for their successful application in biomedicine.
Used for many years for the synthesis of many classes of drugs, in the last two
decades the phenothiazine derivatives proved a promising potential for the cancer
treatment. Taking into account phenothiazine properties and poly(ethylene glycol)
biocompatibility, a series of three new PEGylated phenothiazine derivatives were
prepared by grafting PEG chains to the phenothiazine core. The structure of the targeted
molecules was confirmed by FTIR and NMR spectroscopy. The capacity of the
synthetized compounds to self-assembly in water was studied by DLS and UV-vis
techniques. Their biocompatibility was assessed on normal human dermal fibroblasts and
five human cancer cell lines. The synthetized compounds proved excellent
biocompatibility on normal cells. A concentration dependent cytotoxicity against cancer
cell lines was noticed for two of synthesis PEGylated phenothiazine derivatives. In vivo
anti-tumor investigations presented high tumor inhibition comparable to traditional drugs.