Improved method for preparing Ni(II) complex of (S)-tyrosine Schiff base and its use in the automated synthesis of O-(2'-[F]fluoroethyl)-l-tyrosine using solid-phase extraction purification.

O-(2'-[F]fluoroethyl)-l-tyrosine is reportedly suitable for PET-imaging of brain tumours. We report here the synthesis of Ni(II)-complex of Schiff's base (S)-[N-2-(N'-benzylprolyl)amino]-benzophenone,((S)BPB) and alkylated l-tyrosine precursor, Ni(II)-(S)-BPB-l-Tyr-O-CH-CH-OTs by an improved method. A fully-automated radio-synthesis including non-HPLC purification was developed with a radio-chemical yield of 24.

A Novel Folate-Targeted Nanoliposomal System of Doxorubicin for Cancer Targeting.

Targeted drug delivery systems for cancer improves anti-tumor efficacy and reduces systemic toxicity by restricting availability of cytotoxic drugs within tumors. Targeting moieties, such as natural ligands (folic acid, transferrin, and biotin) which are overexpressed on tumors, have been used to enhance liposome-encapsulated drug accumulation within tumors and resulted in better control. In this report, we explored the scope of targeting ligand folic acid, which is incorporated in liposome systems using folic acid-modified cholesterol (CPF), enabled highly selective tumor-targeted delivery of liposome-encapsulated doxorubicin and resulted in increased cytotoxicity within tumors.