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1.
Chem Commun (Camb) ; 52(38): 6419-22, 2016 May 11.
Article in English | MEDLINE | ID: mdl-27094457

ABSTRACT

An efficient approach to (Rp) planar-chiral tri- and tetracyclic ortho-condensed aromatic ferrocenes was developed through the enantioselective cationic Au(i)-catalyzed cycloisomerization, in the presence of bidentate phosphine ligand (R)-DTBM-Segphos, from readily available ortho-alkynylaryl ferrocenes under very mild conditions (11 examples, up to 92% yield and 93% ee).

2.
Eur J Med Chem ; 111: 58-71, 2016 Mar 23.
Article in English | MEDLINE | ID: mdl-26854378

ABSTRACT

Photodynamic therapy (PDT) is a minimally invasive procedure that can provide a selective eradication of neoplastic diseases by the combined effect of a photosensitizer, light and oxygen. New amino oligo(phenylene-ethynylene)s (OPEs), bearing hydrophilic glucoside terminations, have been prepared, characterized and tested as photosensitizers in PDT. The effectiveness of these compounds in combination with UVA light has been checked on two tumor cell lines (HEp-2 and HeLa cells, derived from a larynx carcinoma and a cervical carcinoma, respectively). The compounds triggered a mitotic blockage that led to the cell death, being the effect active up to 3 µm concentration. The photophysical properties of OPEs, such as high quantum yield, stability, singlet oxygen production, biocompatibility, easy cell-internalization and very good response even at low concentration, make them promising photosensitizers in the application of PDT.


Subject(s)
Alkynes/pharmacology , Biocompatible Materials/pharmacology , Ethers/pharmacology , Glucose/chemistry , Photochemotherapy , Photosensitizing Agents/pharmacology , Alkynes/chemical synthesis , Alkynes/chemistry , Biocompatible Materials/chemical synthesis , Biocompatible Materials/chemistry , Cell Death/drug effects , Cell Line, Tumor , Dose-Response Relationship, Drug , Ethers/chemical synthesis , Ethers/chemistry , HeLa Cells , Hep G2 Cells , Humans , Molecular Structure , Photosensitizing Agents/chemical synthesis , Photosensitizing Agents/chemistry , Structure-Activity Relationship , Ultraviolet Rays
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