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  • Design, synthesis and in vitro antitumour activity of new heteroaryl ethylenes.

Design, synthesis and in vitro antitumour activity of new heteroaryl ethylenes.

European journal of medicinal chemistry (2011-11-29)
Cosimo G Fortuna, Vincenza Barresi, Carmela Bonaccorso, Giuseppe Consiglio, Salvatore Failla, Angela Trovato-Salinaro, Giuseppe Musumarra
PMID22119128
ABSTRACT

Almond and VolSurf + modelling procedures allowed the structural design of new di- and mono-heteroaryl-ethylenes. The structural modifications suggested by the molecular modelling were verified by the synthesis of the designed molecules and by the evaluation of their in vitro activities against two lung tumour cell lines, A549 and H226. 2-{(E)-2-[5'-(Dibutylamino)-2,2'-bithien-5-yl]vinyl}-1-methylquinolinium iodide exhibited in vitro antiproliferative activity two orders of magnitude higher than that of the most active compound previously synthesized in our laboratory.