Evaluation of in vivo biological activities of tetrapyrrole ethanolamides as novel anticancer agents.

Abstract The tetrapyrrole ethanolamide derivatives, hematoporphyrin propylether ethanolamide (HPPEEA, 1 ) and pheophorbide a ethanolamide (PEA, 2 ) have previously shown some photodynamic activities in an in vitro photodynamic assay (D. Girard et al. Bioorg. Med. Chem. Lett. 18 (2008) 360–365). Extending this study to an in vivo one, HPPEEA and PEA were evaluated for their anticancer, toxicity, and pharmacokinetic activities in mouse animal models. The compounds showed moderate anticancer activity without apparent acute toxicity and without secondary tumour development. This indicates noteworthy anti-metastasis activity. The pharmacokinetic study revealed the compound fast clearances from body tissues. This is an important therapeutic concern since these compounds are light sensitive. Thus, the combination of photodynamic and anti-metastasis activities with fast tissue clearance indicates that HPPEEA and PEA are good candidates for further photodynamic treatment evaluations.