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1.
Chem Commun (Camb) ; 52(38): 6419-22, 2016 May 11.
Artigo em Inglês | MEDLINE | ID: mdl-27094457

RESUMO

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.
Artigo em Inglês | MEDLINE | ID: mdl-26854378

RESUMO

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.


Assuntos
Alcinos/farmacologia , Materiais Biocompatíveis/farmacologia , Éteres/farmacologia , Glucose/química , Fotoquimioterapia , Fármacos Fotossensibilizantes/farmacologia , Alcinos/síntese química , Alcinos/química , Materiais Biocompatíveis/síntese química , Materiais Biocompatíveis/química , Morte Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Relação Dose-Resposta a Droga , Éteres/síntese química , Éteres/química , Células HeLa , Células Hep G2 , Humanos , Estrutura Molecular , Fármacos Fotossensibilizantes/síntese química , Fármacos Fotossensibilizantes/química , Relação Estrutura-Atividade , Raios Ultravioleta
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